AUTHOR OF THIS BLOG

DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER

Scientific Update, UK, Course on ‘Chemical Development & Scale Up in the Pharmaceutical Industry’, Sea Princess Hotel, Mumbai, India, 6– 8th Feb 2017

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Scientific Update, UK,  Course on ‘Chemical Development & Scale Up in the Pharmaceutical Industry’, Sea Princess Hotel, Mumbai, India, 6th – 8th February 2017

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6-8 FEB 2017

 

 

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Scientific Update, UK,  Course on ‘Chemical Development & Scale Up in the Pharmaceutical Industry’, Sea Princess Hotel, Mumbai, India, 6th – 8th February 2017……..Chemical process development is generally not taught as part of degree courses in higher education; the conversion of a synthetic route used for making milligram or gram quantities of a chemical into a process for manufacturing multi-kilogram and tonne quantities is typically learnt “on the job” by chemists in industry. For many years, little chemical development work was published in the literature, until the establishment of the Organic Process R & D journal by Dr Trevor Laird (Founder of Scientific Update). Even now, “tricks of the trade” are handed down within individual company organisations, and it can be difficult to gain an awareness of what is involved in chemical development, and of the skills and techniques required to efficiently scale up chemical processes.

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This three-day course, written and presented by highly experienced process chemists from the pharmaceutical and fine chemical industry, provides a comprehensive overview of this fascinating and important element of the chemical industry. A logical investigative approach to all aspects of chemical development is described, with an abundance of case studies from literature, conferences and private communications. The multi-disciplinary nature of chemical development is emphasised, from the initial interaction with laboratory research scientists to the vital partnership with chemical engineers in the pilot plant and in the production environment. The lectures are interspersed with interactive problem sessions, enabling participants to share in the problem solving and troubleshooting typically experienced during chemical development.

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TRAINING COURSES

EVENT

Title:Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries

Subtitle:Principles and Practice

When:06.02.2017 – 08.02.2017

Tutors:

John Knight

Will Watson

Where:The Sea Princess Hotel – MumbaiBrochure  View Brochure  6-8 FEB 2017

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THE SEA PRINCESS HOTEL

DESCRIPTION

AT THE END OF THE COURSE PARTICIPANTS WILL HAVE GAINED:

  • A logical investigative approach to chemical development and optimisation.
  • An insight into the factors involved in development and scale-up.
  • An appreciation of chemical engineering concepts, particularly mixing, heat transfer and process control.
  • A preliminary knowledge of statistical methods of optimisation.
  • Improved ability to decide which parts of the chemical process to examine in detail
  • Ideas for efficient resource allocation
  • Improved troubleshooting and problem solving ability

Kind regards,

Claire Francis

Dr Claire Francis

Director

Scientific Update Ltd, Maycroft Place

Stone Cross, Mayfield, East Sussex

TN20 6EW, UK

T: +44 (0) 1435 873062

E: claire@scientificupdate.co.uk

W: www.scientificupdate.co.uk

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WO 2016181414, IVACAFTOR, NEW PATENT, COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

 PATENTS  Comments Off on WO 2016181414, IVACAFTOR, NEW PATENT, COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Nov 242016
 

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CSIR, Dr. D. Srinivasa Reddy

WO2016181414, PROCESS FOR THE SYNTHESIS OF IVACAFTOR AND RELATED COMPOUNDS

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2016181414&recNum=1&maxRec=&office=&prevFilter=&sortOption=&queryString=&tab=PCTDescription

REDDY, Dumbala Srinivasa; (IN).
NATARAJAN, Vasudevan; (IN).
JACHAK, Gorakhnath Rajaram; (IN)

COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH [IN/IN]; Anusandhan Bhawan, Rafi Marg New Delhi 110001 (IN)

The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R1, R2, R3, R4, R5, R6, R7 and Ar1are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides

See Eur J Org Chem, Nov 2015, for an article by the inventors, describing a process for preparing ivacaftor using 4-quinolone-3-carboxylic acid amides. The inventors appear to be based at National Chemical Laboratories of CSIR.

Ivacaftor, also known as N-(2,4-di-tert-butyl-5-hydroxyphenyl)-l,4-dihydro-4-oxoquinoline-3-carboxamide, having the following Formula (A):

Formula (A)

[003] Ivacaftor was approved by FDA and marketed by vertex pharma for the treatment of cystic fibrosis under the brand name KALYDECO® in the form of 150 mg oral tablets. Kalydeco® is indicated for the treatment of cystic fibrosis in patients age 6 years and older who have a G55ID mutation in the CFTR (cystic fibrosis transmembrane conductance regulator)gene.

[004] U.S. 20100267768 discloses a process for preparation of ivacaftor, which involves the coupling of 4-oxo-l,4-dihydro-3- quinoline carboxylic acid with hydroxyl protected phenol intermediate in the presence of propyl phosphonic anhydride (T3P®) followed by deprotection of hydroxyl protection group and optional crystallization with isopropyl acetate. The publication also discloses the use of highly expensive coupling reagent, propyl phosphonic anhydride; which in turn results to an increase in the manufacturing cost. The process disclosed is schematically represented as follows:

[005] Article titled “Discovery of N-(2,4-Di-te -butyl-5-hydroxyphenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide (VX-770, Ivacaftor), a Potent and Orally Bioavailable CFTR Potentiator” byHadida,S et. al in . Med. Chem., 2014, 57 (23), pp 9776-9795 reportsN-(2,4-di-teri-butyl-5-hydroxyphenyl)-4-oxo- 1 ,4-dihydroquinoline-3-carboxamide (VX-770, 48, ivacaftor), an investigational drug candidate approved by the FDA for the treatment of CF patients 6 years of age and older carrying the G551D mutation.

[006] WO 2014125506 A2 discloses a process for the preparation of ivacaftor in high yield and purity by using novel protected quinolone carboxylic acid compounds as intermediates.

[007] Article titled “Expeditious synthesis of ivacaftor” by Jingshan Shen et. al in Heterocycles, 2014, 89 (4), pp 1035 – 1040 reports an expeditious synthesis for ivacaftor featuring modified Leimgruber-Batcho procedure. The overall yield is 39% over six steps from commercially available 2-nitrobenzoyl chloride.

[008] U.S.2011/064811 discloses a process for preparation of ivacaftor, which involves condensation of 4-oxo-l,4-dihydro-3- quinolone carboxylic acid with 5- amino-2,4-di-(tert-butyl)phenol in the presence of HBTU followed by the formation of ethanol crystalate, which is then treated with diethyl ether to yield ivacaftor as a solid.

[010] U.S. 7,495,103 discloses modulators of ATP-binding cassette transporters such as ivacaftor and a process for the preparation of modulators of ATP-binding cassette transporters such as quinolone compounds. The process includes condensation of 4-oxo-l,4-dihydro-3 -quinolone carboxylic acid with aniline in presence of 2-(lH-7-azabenzotriazol-l-yl)-l,l,3,3-tetramethyluronium hexafluoro phosphate methanaminium (HATU) as shown:

[011] U.S. 2011/230519 discloses a process for preparation of 4-oxo-l,4-dihydro-3-quinoline carboxylic acid by reaction of aniline with diethylethoxymethylenemalonate at 100-110°C followed by cyclization in phenyl ether at temperature 228-232°C and then hydrolysis, as shown below:

[012] US 7,402,674 B2 discloses 7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments.

[013] US 4,981,854 discloses l-aryl-4-quinolone-3 carboxylic acids, processes for their preparation and anti-bacterial agents and feed additives containing these compounds.

Article titled “Ozonolysis Applications in Drug Synthesis” by Van Ornum,S.G. ; Champeau,R.M.; Pariza,R. in Chem. Rev., 2006, 106 (7), pp 2990-3001 reports that ozonolysis for the synthesis of numerous interesting bioactive natural products and pharmaceutical agents.

[014] Article titled “Safe Execution of a Large-Scale Ozonolysis: Preparation of the Bisulfite Adduct of 2-Hydroxyindan-2-carbox-aldehyde and Its Utility in a Reductive Animation” by RaganJ.A. et. al. in Org. Proc. Res. Dev., 2003, 7 (2), pp 155-160 reports various routes to bisulfite adduct, the most efficient of which involved vinyl Grignard addition to 2-indanone followed by ozonolysis and workup with aqueous NaHS03 to effect reduction and bisulfite formation in a single pot. The utility of bisulfite adduct is as an aldehyde surrogate in a reductive amination reaction.

[015] The reported methods for the synthesis of ivacaftor suffered from several drawbacks such as harsh conditions, high temperature reactions and use of large excess of polyphosphoric acid and corrosive phosphoryl chloride etc. Furthermore, synthesis of ivacaftor requires use of high performance liquid chromatography (HPLC) techniques for the separation of ivacaftor and their analogues.

[016] Therefore, development of a simple and efficient synthetic route is in urgent need. Accordingly the present inventors developed environmentally benign, cost effective and short synthetic route for the synthesis of ivacaftor and their analogues.

Example 1:

Procedur A:

To a solution of indole acetic acid (500 mg, 2.85 mmol), aniline (2.85 mmol), HOBt (3.4 mmol) in acetonitrile (10 mL), EDC.HCl (3.4 mmol) followed by DIPEA (11.4 mmol) was added, and mixture was stirred for 16 h at ambient temperature. The

reaction mixture was evaporated to dryness, diluted with EtOAc (25 mL), washed with saturated aqueous NaHC03 solution (5 mL), H20 (5 mL), brine (5 mL), and dried over Na2S04. The crude material obtained after removal of solvent was purified by column chromatography (silica gel 230-400 mesh, ethyl acetate – pet ether) to afford corresponding amide as a colorless solid.

[040] Example 2:

2-(lH-indol-3-yl)-N-phenylacetamide (1) :

Yield: 570 mg; 80%; 1H NMR (200MHz, DMSO-d6) δ = 10.95 (brs, 1 H), 10.14 (s, 1 H), 7.64 (d, J = 7.8 Hz, 3 H), 7.47 – 7.24 (m, 4 H), 7.21 – 6.92 (m, 3 H), 3.76 (s, 2H); MS: 273 (M+Na)+.

[041] Example 3:

5-(2-(lH-indol-3-yl)acetamido)-2,4-di-tert-butylphenyl methyl carbonate (2): Yield: 800 mg; 64%; 1H NMR (200 MHz, DMSO-d6) δ = 11.51 (brs, 1 H), 9.41 (s, 1 H), 8.12 (d, J = 7.6 Hz, 1 H), 7.96 – 7.78 (m, 3 H), 7.71 – 7.42 (m, 3 H), 4.34 (s, 3 H), 4.30 (s, 2 H), 1.79 (s, 9 H), 1.64 (s, 9 H); MS: 459 (M+Na)+.

[042] Example 4:

(S)-2-(lH-indol-3-yl)-N-(l-phenylethyl)acetamide (3):

Yield: 620 mg; 78%; 1H NMR (400MHz ,DMSO-d6)5 = 10.88 (brs, 1 H), 8.48 (d, J = 8.1 Hz, 1 H), 7.59 (d, J = 7.8 Hz, 1 H), 7.39 – 7.26 (m, 5 H), 7.25 – 7.16 (m, 2 H), 7.08 (t, J = 7.3 Hz, 1 H), 7.02 – 6.95 (m, 1 H), 4.96 (t, J = 7.3 Hz, 1 H), 3.59 (s, 2H), 1.38 (d, J = 7.1 Hz, 3 H).

[043] Example 5:

N-(4-Fluorophenyl)-2-(lH-indol-3-yl)acetamide (4):

1H NMR (400 MHz, DMSO-d6) : δ 10.93 (brs, 1H), 10.17 (s, 1H), 7.68 – 7.61 (m, 3H), 7.36 (d, J= 8.1 Hz, 1H), 7.27 (d, J= 2.0 Hz, 1H), 7.15 – 7.13 (m, 3H), 7.11 – 6.99 (m, 1H), 3.73 (s, 2H); 13C NMR (100 MHz, DMSO-d6) : δ 170.1, 159.5, 157.1, 136.6, 136.3, 127.7, 124.4, 121.5, 121.3, 121.2, 119.1, 118.9, 115.8, 115.6, 111.8, 108.9, 34.2; MS: 269 (M+H)+

[044] Example 6:

N-(4-Chlorophenyl)-2-(lH-indol-3-yl)acetamide (5):

1H NMR (200 MHz, DMSO-d6): 510.93 (brs, 1H),10.24 (s, 1H), 7.67 – 7.59 (m, 3H), 7.36 – 7.27 (m, 4H), 7.12 – 6.98 (m, 2H), 3.74 (s, 2H); 13CNMR (100 MHz, DMSO-d6): 5170.4, 138.9, 136.7, 129.1, 127.8, 127.1, 124.5, 121.6, 121.2, 119.2, 119.0, 115.7, 111.9, 108.9, 34.3; MS: 285 (M+H)+.

[045] Example 7:

2-(lH-Indol-3-yl)-N-(p-tolyl)acetamide (6) :

1H NMR (400 MHz, DMSO-d6): 510.91 (brs, 1H), 10.01 (s, 1H), 7.62 (d, J= 7.8 Hz, 1H), 7.50 (d, J= 8.6 Hz, 2H), 7.37 (d, J= 8.1 Hz, 1H), 7.29 – 7.26 (m, 1H), 7.10 – 7.07 (m, 3H), 7.01 – 6.99 (m, 1H), 3.71 (s, 2H), 2.23 (s, 3H); 13C NMR (100 MHz, DMSO-de): 5170.0, 137.4, 136.6, 132.4, 129.5, 127.7, 124.3, 121.4, 119.6, 119.2, 118.8, 111.8, 109.1, 34.2, 20.9; MS: 265 (M+H)+.

[046] Example 8:

N-(4-Ethylphenyl)-2-(lH-indol-3-yl)acetamide (7):

XH NMR (400 MHz, DMSO-d6): 510.91 (brs, 1H), 10.01 (s, 1H), 7.61 (s, 1H), 7.52 (d, J= 8.3 Hz, 2H), 7.36 (d, J= 8.1 Hz, 1H), 7.26 (s, 1H), 7.15 – 7.04 (m, 3H), 6.99 (s, 1H), 2.55 (t, J= 7.5 Hz, 2H), 1.15 (t, J= 7.5 Hz, 3H); 13C NMR (100 MHz, DMSO-d6): 5169.9, 138.9, 137.6, 136.6, 128.3, 127.7, 124.3, 121.4, 119.6, 119.2, 118.8, 111.8, 109.1, 40.6, 40.4, 40.2, 40.0, 39.8, 39.6, 39.4, 34.2, 28.0, 16.2; MS: 279 (M+H)+.

[047] Example 9:

2-(lH-Indol-3-yl)-N-(4-propylphenyl)acetamide (8):

1H NMR (400 MHz, DMSO-d6): 58.48 (brs, 1H), 7.64 (d, J = 8.1 Hz, 1H), 7.50 – 7.42 (m, 2H), 7.33 – 7.15 (m, 6H), 7.07 (d, J= 8.3 Hz, 2H), 3.92 (s, 2H), 2.52 (t, J= 7.6 Hz, 2H), 1.65 – 1.53 (m, 2H), 0.91 (t, J= 7.3 Hz, 3H); 13C NMR (100 MHz, DMSO-d6): 5169.7, 138.9, 136.5, 135.2, 128.8, 126.9, 124.0, 122.8, 120.4, 120.1, 118.7, 111.6, 108.7, 37.4, 34.5, 24.6, 13.7; MS: 315 (M+Na)+.

[048] Example 10:

2-(lH-Indol-3-yl)-N-(4-isopropylphenyl)acetamide (9) :

yield 79% ; 1H NMR (400 MHz, DMSO-d6): δ 10.91 (brs, 1H), 10.01 (s, 1H), 7.62 (d, = 7.8 Hz, 1H), 7.55 – 7.49 (m, = 8.6 Hz, 2H), 7.37 (d, = 8.1 Hz, 1H), 7.26 (d, = 2.0 Hz, 1H), 7.18 – 7.11 (m, = 8.6 Hz, 2H), 7.11 – 7.05 (m, 1H), 7.02 – 6.95 (m, 1H), 2.95 – 2.71 (m, 1H), 1.17 (d, = 6.8 Hz, 6H); 13C NMR (100 MHz, DMSO-d6): δ 169.9, 143.5, 137.6, 136.6, 127.7, 126.8, 124.3, 121.4, 119.7, 119.2, 118.8, 111.8, 109.2, 24.4; MS: 315 (M+Na)+.

[049] Example 11:

2-(lH-indol-3-yl)-N-(4-(trifluoromethoxy)phenyl)acetamide (10):

Yield 85% ; 1H NMR (400 MHz, CDC13): δ 8.35 (brs., 1 H), 7.44 – 7.38 (m, 2 H), 7.27 – 7.21 (m, 3 H), 7.12 – 7.05 (m, 1H), 7.03 – 6.95 (m, 2H), 6.93 (d, = 8.6 Hz, 2H), 3.75 (s, 2H); 13C NMR (100 MHz, CDC13): δ 170.0, 145.3, 136.5, 136.2, 126.8, 124.1, 123.0, 121.6, 121.2, 120.5, 118.5, 111.7, 108.2, 34.4; MS: 335 (M+Na)+.

[050] Example 12:

N-(2-chloro-5-methoxyphenyl)-2-(lH-indol-3-yl)acetamide (11):

Yield 75% ; XH NMR (200 MHz, DMSO-d6): δ 10.98 (brs, 1H), 9.27 (s, 1H), 7.59 (d, = 7.8 Hz, 1H), 7.53 (d, = 2.9 Hz, 1H), 7.39 – 7.32 (m, 3H), 7.09 – 6.99 (m, 2H), 6.74 (dd, = 3.0, 8.8 Hz, 1H), 3.85 (s, 2H), 3.71 (s, 3H); 13C NMR (400 MHz, DMSO-d6): δ 170.4, 160.1, 141.1, 136.7, 130.0, 127.8, 124.4, 121.6, 119.2, 119.0, 111.9, 109.1, 105.4, 55.4, 34.4; MS: 315 (M+Na)+.

[051]Example 13:

N-(2-ethylphenyl)-2-(lH-indol-3-yl)acetamide (12):

Yield 78% ; 1H NMR (400 MHz, CDC13): δ 8.68 (brs, 1H), 7.95 (d, = 8.1 Hz, 1H), 7.67 (d, = 7.8 Hz, 1H), 7.48 – 7.44 (m, 2H), 7.29 – 7.23 (m, 1H), 7.22 – 7.20 (m, 3H), 7.05 (d, = 4.4 Hz, 2H), 2.00 (q, = 7.4 Hz, 2H), 0.67 (t, = 7.6 Hz, 3H); 13C NMR (100 MHz, CDC13): δ 169.9, 136.6, 135.0, 134.3, 128.7, 126.7, 125.1, 124.1, 123.0, 122.5, 120.4, 118.7, 111.6, 108.6, 34.4, 24.2, 13.6.

[052] Example 14:

N-(2-bromophenyl)-2-(lH-indol-3-yl)acetamide(13):

Yield 76%; 1H NMR (200 MHz, DMSO-d6): δ 11.00 (brs, 1H), 9.30 (s, 1H), 7.81 -7.77 (m, 1H), 7.63 – 7.56 (m, 2H), 7.41 – 7.35 (m, 3H), 7.11 – 7.05 (m, 3H), 3.85 (s, 2H);13C NMR (100 MHz, DMSO-d6): δ 169.9, 136.2, 132.5, 128.0, 127.2, 126.4, 125.5, 124.4, 121.2, 118.7, 118.5, 116.4, 111.4, 108.0, 33.2.

[053] Example 15:

N-benzyl-2-(lH-indol-3-yl)acetamide (14):

Yield 85%; 1H NMR (400 MHz, DMSO-d6): δ 10.89 (brs., 1H), 8.40 (t, = 5.7 Hz, 1H), 7.57 (d, = 7.8 Hz, 1H), 7.36 (d, = 8.1 Hz, 1H), 7.32 – 7.18 (m, 6H), 7.08 (t, = 7.5Hz, 1H), 7.03 – 6.90 (m, 1H), 4.28 (d, = 5.9Hz, 2H), 3.60 (s, 2H); 13C NMR (100 MHz, DMSO-de): δ 171.2, 140.1, 136.6, 128.7, 127.7, 127.2, 124.3, 121.4, 119.2, 118.7, 111.8, 109.3, 42.7, 33.2.

[054] Example 16:

2-(lH-indol-3-yl)-N-(4-methoxybenzyl)acetamide(15):

Yield 85% ; 1H NMR (400 MHz, DMSO-d6): δ 10.87 (brs, 1 H), 8.32 (t, = 5.6 Hz, 1 H), 7.55 (d, = 7.8 Hz, 1H), 7.35 (d, = 8.1 Hz, 1H), 7.22 – 7.13 (m, 3H), 7.11 – 7.05 (m, 1 H), 7.00 – 6.94 (m, 1H), 6.84 (d, = 8.6 Hz, 2H), 4.20 (d, = 6.1 Hz, 2H), 3.72 (s, 3H), 3.56 (s, 2H); 13C NMR (100 MHz, DMSO-d6): δ 171.1, 158.6, 136.6, 132.0, 129.0, 127.7, 124.2, 121.4, 119.2, 118.7, 114.1, 111.8, 109.4, 55.5, 42.1, 33.2.

[055] Example 17:

N,N-dibenzyl-2-(lH-indol-3-yl)acetamide (16):

Yield 70% ; 1H NMR (400 MHz, DMSO-d6): δ 10.91 (brs, 1H), 7.50 (d, = 7.8 Hz, 1H), 7.37 – 7.34 (m, 3H), 7.30 (d, = 6.6 Hz, 1H), 7.25 – 7.19 (m, 3H), 7.17 (t, = 6.6 Hz, 5H), 7.16 (d, = 7.8 Hz, 1H), 7.00 – 6.97 (m, 1H), 4.59 (s, 2H), 4.50 (s, 2H), 3.86 (s, 2H); 13C NMR (100 MHz, DMSO-d6): δ 171.7, 138.2, 136.6, 129.2, 128.8, 128.1, 127.8, 127.7, 127.5, 127.1, 124.2, 121.5, 119.2, 118.8, 111.8, 108.5, 50.7, 48.4, 31.2.

[056] Example 18:

2-(lH-indol-3-yl)-N-propylacetamide (17):

Yield 75% ; XH NMR (200 MHz, DMSO-d6): δ 10.86 (brs, 1H), 7.88 – 7.80 (m, 1H), 7.56 (d, = 7.6 Hz, 1H), 7.31 (d, = 7.8 Hz, 1H), 7.17 (d, = 2.3 Hz, 1H), 7.06 – 6.92 (m, 2H), 3.48 (s, 2H), 3.00 (q, J = 6.8 Hz, 2H), 1.39 (sxt, / = 7.2 Hz, 2H), 0.88 – 0.75 (t, = 7.2 Hz, 3H); 13C NMR (100 MHz, DMSO-d6): δ 171.0, 136.6, 127.8, 124.2,

121.4, 119.2, 118.7, 111.8, 109.6, 39.4, 33.3, 22.9, 11.9.

[057] Example 19:

N-hexyl-2-(lH-indol-3-yl)acetamide (18) :

Yield 87% ; 1H NMR (400 MHz, DMSO-d6): δ 10.84 (brs, 1H), 7.83 (brs, 1H), 7.54 (d, = 7.8 Hz, 1H), 7.33 (d, = 8.1 Hz, 1H), 7.21 – 7.13 (m, 1H), 7.06 (t, = 7.6 Hz, 1H), 6.96 (t, J = 7.5 Hz, 1H), 3.47 (s, 2H), 3.03 (q, / = 6.8 Hz, 2H), 1.37 (t, = 6.5 Hz, 2H), 1.30 – 1.15 (m, 6H), 0.84 (t, = 6.7 Hz, 3H); 13C NMR (100 MHz, DMSO-d6): δ 170.9, 136.6, 127.7, 124.2, 121.3, 119.1, 118.7, 111.7, 109.5, 39.06, 33.2, 31.5, 29.6, 26.5, 22.5, 14.4.

[058] Example 20:

Methyl (2-(lH-indol-3-yl)acetyl)-L-alaninate (19):

Yield 79% ; 1H NMR (400 MHz, CDC13): δ 8.53 (brs, 1H), 7.60 (d, = 7.8 Hz, 1H), 7.41 (d, = 8.1 Hz, 1H), 7.25 – 7.23 (m, 1H), 7.19 – 7.14 (m, 2H), 6.27 (d, = 7.3 Hz, 1H), 4.63 (t, = 7.3 Hz, 1H), 3.78 (s, 2H), 3.68 (s, 3H), 1.31 (d, = 7.3 Hz, 3H); 13C NMR (100 MHz, CDC13): δ 173.4, 171.2, 136.4, 127.0, 123.8, 122.5, 119.9, 118.7,

111.5, 108.5, 52.4, 48.0, 33.3, 18.2.

[059] Example 21:

-(6-chloro-lH-indol-3-yl)-N-phenylacetamide(20):

To a solution of 6-Chloro indole 20a (300 mg, 1.98 mmol )in anhydrous THF, Oxalyl chloride (186 μΤ, 276 mg, 2.18 mmol) was added and the mixture stirred at room temperature. After 2 h, N,N-Diisopropylethylamine (758 μΤ, 562 mg, 4.35 mmol) was

introduced to the mixture, followed by the aniline (221.0 mg, 2.37 mmol). The temperature was raised to 45 °C, and heating continued for 18 h. The solvent was evaporated, and then mixture was diluted with EtOAC (15 mL), washed with brine and dried over anhydrous Na2S04. The crude material obtained after removal of solvent was purified by column chromatography (10 – 20% EtOAc : Petroleum ether) to afford 20b (295 mg, 51% yield) as a yellow coloured solid. IR Omax(film): 3346, 3307,2853, 1724, 1678 cm“1; 1H NMR (400 MHz, DMSO-d6): δ 12.40 (br. s., 1H), 10.68 (s, 1H), 8.79 (d, = 3.2 Hz, 1H), 8.25 (d, = 8.6 Hz, 1H), 7.85 (d, = 7.8 Hz, 2H), 7.62 (d, = 1.7 Hz, 1H), 7.41 – 7.30 (m, 3H), 7.19 – 7.13 (m, 1H); 13C NMR (100 MHz, DMSO-d6): δ 182.5, 162.5, 140.0, 138.4, 137.4, 129.2, 128.5, 125.4, 124.8, 123.4, 122.9, 120.8, 113.0, 112.3; HRMS (ESI) Calculated for Ci6HnN2OCl[M+H]+: 299.0582, found 299.0580;

A solution of 20b (300 mg, 0.99 mmol) dissolved in MeOH (40 mL) was added to NaBH4 (45 mg, 1.23 mmol). The reaction was stirred for 4h and then added to saturated solution of Na2S04. The reaction mixture was further stirred for lh and then filtered through Celite.The filtrate obtained was concentrated in vacuo, and then mixture was diluted with EtOAc (15 mL), washed with brine and dried over anhydrous Na2S04. The crude material obtained after removal of solvent was forwarded for next step without further purification.In an N2 atmosphere, TMSC1 (1.272 mL, 9.9 mmol) in CH3CN (40 mL) was added to sodium iodide (1.488 mg, 9.9 mmol) and stirred for 2h. The reaction mixture was cooled to 0 °C and a solution of above crude alcohol (0.99 mmol) in CH3CN (10 mL) was then added drop wise over 30 min, followed by stirring for 3h. The reaction mixture was poured into NaOH (7g in 40 mL of water) and then extracted with ethyl acetate (15×2). The organic layer was washed with aq.Na2S203, dried over Na2S04 and concentrated in vacuo. The residue was chromatographed on silica gel (EtOAc:Pet ether) to afford 20 as a off white solid (two steps 38 % ); IR Umax(film): 3273, 3084,2953, 2857, 1629, 1562 cm“1; 1H NMR (400 MHz, DMSO-d6): δ 11.06 (br. s., 1H), 10.13 (br. s., 1H), 7.62 – 7.57 (m, 3H), 7.40 (s, 1H), 7.30 – 7.25 (m, 3H), 7.04 – 6.99 (m, 2H), 3.71 (s, 2H); 13C NMR (100 MHz, DMSO-d6): δ 170.1,

139.7, 136.9, 129.2, 126.5, 126.3, 125.5, 123.7, 120.6, 119.6, 119.3, 111.5, 109.4, 34.0; HRMS (ESI):Calculated for Ci6Hi4N2OCl[M+H]+: 285.0789, found 285.0786.

[060] Example 22:

2-(5-chloro-lH-indol-3-yl)-N-phenylacetamide(21):

21a 21b 21

To a solution of 5-Chloro indole 21a (300 mg, 1.98 mmol )in anhydrous THF(20 mL), Oxalyl chloride (186 ^L, 276 mg, 2.18 mmol) was added and the mixture stirred at room temperature. After 2 h, N,N-diisopropylethylamine (758 μΕ, 562 mg, 4.35 mmol) was introduced to the mixture, followed by the aniline (221.0 mg, 2.37 mmol). The tempera ture was raised to 45 °C, and heating continued for 18 h. The solvent was evaporated, and then mixture was diluted with EtOAC (15 mL), washed with brine and dried over anhydrous Na2S04. The crude material obtained after removal of solvent was purified by column chromatography (10 – 20% EtOAc : Petroleum ether) to afford (21b) (305 mg, 53% yield) as a yellow coloured solid. IR rjmax(film): 3346, 3307,2853, 1724, 1678 cm“1; 1H NMR (400 MHz, DMSO-d6): δ 12.40 (br. s., 1H), 10.68 (s, 1H), 8.79 (d, = 3.2 Hz, 1H), 8.25 (d, = 8.6 Hz, 1H), 7.85 (d, = 7.8 Hz, 2H), 7.62 (d, = 1.7 Hz, 1H), 7.42 – 7.30 (m, 3H), 7.20 – 7.14 (m, 1H); 13C NMR (100 MHz, DMSO-d6): δ 182.4, 162.4, 140.3, 138.4, 135.4, 129.2, 127.9, 124.8, 124.1, 120.8, 114.8, 112.0; HRMS (ESI) Calculated for Ci6HnN2OCl[M+H]+: 299.0582, found 299.0580; A solution of 21b (200 mg, 0.66 mmol) dissolved in MeOH (30 mL) was added to NaBH4 (30 mg, 0.82 mmol). The reaction was stirred for 4h and then added to saturated solution of Na2S04. The reaction mixture was further stirred for lh and then filtered through Celite. The filtrate obtained was concentrated in vacuo, and then mixture was diluted with EtOAc (15 mL), washed with brine and dried over anhydrous Na2S04. The crude material obtained after removal of solvent was forwarded for next step without further purification. In an N2 atmosphere, TMSC1 (848 mL, 6.6 mmol) in CH3CN (25 mL) was added to sodium iodide (992 mg, 6.6 mmol) and stirred for 2h. The reaction mixture was cooled to 0 °C and a solution of above crude alcohol(0.66 mmol) in CH3CN (5 mL) was then added dropwise over 30 min, followed by stirring for 3h. The reaction mixture was poured into NaOH (5g in 30 mL of water) and then extracted with ethyl acetate(15×2). The organic layer was washed with aq.Na2S203, dried over Na2S04 and concentrated in vacuo. The residue was chromatographed on silica gel (EtOAc:Pet ether) to afford 22 as a off white solid (two steps 42 % ); IR Umax(film): 3273, 3084,2955, 2857, 1629, 1562 cm“1; 1H NMR (400 MHz, DMSO-d6): δ 11.13 (br. s., 1H), 10.11 (s, 1H), 7.67 (s, 1H), 7.60 (d, = 7.8 Hz, 2H), 7.39 – 7.27 (m, 4H), 7.13 – 7.02 (m, 2H), 3.16 (s, 2H); 13C NMR (100 MHz, DMSO-d6): δ 169.9, 139.8, 135.0, 129.2, 128.9, 126.2, 123.6, 121.4, 119.6, 118.6, 113.4, 109.0, 34.0; HRMS (ESI) Calculated for Ci6H14N2OCl[M+H]+: 285.0789, found 285.0786.

[061] Example 23:

2-(l-benzyl-lH-indol-3-yl)-N-phenylacetamide (22):

Yield 79% ; 1H NMR (400 MHz, DMSO-d6): δ 7.67 (d, = 7.8 Hz, 1H), 7.54 (brs, 1H), 7.43 – 7.31 (m, 6H), 7.31 – 7.25 (m, 3H), 7.23 – 7.15 (m, 4H), 7.12 – 7.06 (m, 1H), 5.36 (s, 2H), 3.91 (s, 2H); 13C NMR (100 MHz, DMSO-d6): δ 169.7, 137.7, 137.2, 137.0, 128.9, 128.9, 127.9, 127.6, 126.9, 124.3, 122.7, 120.2, 119.9, 119.0, 110.2, 107.9, 77.4, 77.1, 76.8, 50.1, 34.5.

[062] Example 24:

Procedure B:

2-(lH-indol-3-yl)-N-phenylacetamidel(100 mg; 0.4 mmol) was dissolved in DCM:MeOH(50 mL; 5: 1), then a stream of 03 was passed through the solution until a blue color developed (10 min). The 03 stream was continued for 4 min. Then surplus O3 was removed by passing a stream of 02 through the solution for 10 min or until the blue colorcompletely vanished. Afterwards pyridine (0.1 mL;1.2mmol) was added to the cold (- 78 °C) mixture. The mixture was allowed to warm to room temperature (1 h) and then Et3N (0.35 mL; 2.4 mmol) were added. After stirring at room temperature overnight the reaction mass was concentrated under reduced pressure to dryness, diluted with EtOAc (30 mL), washed with H20 (5 mL), brine (5 mL), and dried over Na2S04. The crude material obtained after removal of solvent was purified by column chromatography (silica gel 230-400 mesh, MeOH – DCM) to give desired quinolone carboxamide as colorless solid.

[063] Example 25:

4-oxo-N-phenyl-l,4-dihydroquinoline-3-carboxamide (23):

Yield: 65 mg; 62%; XH NMR (200MHz ,DMSO-d6) δ = 12.97 (brs, 1 H), 12.49 (s, 1 H), 8.89 (s, 1 H), 8.33 (d, J = 8.2 Hz, 1 H), 7.91 – 7.69 (m, 4 H), 7.62 – 7.50 (m, 1 H), 7.37 (t, J = 7.8 Hz, 2 H), 7.18 – 7.01 (m, 1 H); MS: 287 (M+Na)+.

[064] Example 26:

2,4-di-tert-butyl-5-(4-oxo-l,4-dihydroquinoline-3-carboxamido)phenyl methyl carbonate (24):

Yield: 35 mg; 34%; 1H NMR (400MHz ,DMSO-d6) δ = 12.96 (brs, 1 H), 12.08 (s, 1 H), 8.94 – 8.82 (m, 1 H), 8.44 – 8.28 (m, 1 H), 7.86 – 7.79 (m, 1 H), 7.78 – 7.73 (m, 1 H), 7.59 (s, 1 H), 7.53 (t, J = 7.5 Hz, 1 H), 7.39 (s, 1 H), 3.86 (s, 3 H), 1.46 (s, 9 H), 1.32 (s, 9 H).

[065] Example 27:

(S)-4-oxo-N-(l-phenylethyl)-l,4-dihydroquinoline-3-carboxamide (25):

Yield: 56 mg; 53%; 1H NMR (500MHz ,DMSO-d6) δ = 12.75 (brs, 1H), 10.54 (d, J = 7.6 Hz, 1H), 8.73 (brs, 1H), 8.28 (d, J = 7.9 Hz, 1H), 7.78 (d, J = 7.9 Hz, 1H), 7.73 -7.68 (m, 1 H), 7.50 (t, J = 7.5 Hz, 1 H), 7.42 – 7.34 (m, 4 H), 7.29 – 7.23 (m, 1 H), 5.18 (t, J = 7.2 Hz, 1 H), 1.50 (d, J = 6.7 Hz, 3 H).

[066] Example 28:

Synthesis of ivacaftor (26):

To a solution of 2,4-di-tert-butyl-5-(4-oxo-l,4-dihydroquinoline-3-carboxamido)phenyl methyl carbonate 5 (30 mg, 0.06mmol) in MeOH (2 mL) was added NaOH (5.3 mg, 0.13mmol) dissolved in H20 (2 mL), and the reaction mixture was stirred at room temperature for 5h. Reaction mass was evaporated to one third of its volume (temperature not exceeding 40°C) and acidified with aq.2N HC1 to pH 2-3. The resulting precipitate was collected by suction filtration give desired compound 7 (19 mg, 76%) as off white solid H NMR (400MHz ,DMSO-d6) δ = 12.88 (d, J = 6.6 Hz, 1 H), 11.81 (s, 1 H), 9.20 (s, 1 H), 8.86 (d, J = 6.6 Hz, 1 H), 8.32 (d, J = 7.8 Hz, 1 H), 7.88 – 7.65 (m, 2 H), 7.51 (t, J = 7.5 Hz, 1 H), 7.16 (s, 1 H), 7.10 (s, 1 H), 1.38 (s,9H), 1.36 (s, 9H).

[067] Example 29:

N-(4-fluorophenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide (27):

Yield 56% ; 1H NMR (400 MHz, DMSO-d6): δ 12.96 (br. s., 1H), 12.50 (s, 1H), 8.88 (s, 1H), 8.33 (d, = 7.3 Hz, 1H), 7.86 – 7.72 (m, 4H), 7.54 (t, = 7.3 Hz, 1H), 7.20 (t, = 8.8 Hz, 2H); 13C NMR (400 MHz, DMSO-d6): δ 176.8, 163.2, 159.7, 157.3, 144.6, 139.6, 135.7, 133.5, 126.4, 125.9, 125.8, 121.8, 119.7, 116.1, 115.9, 110.9.

[068] Example 30:

N-(4-chlorophenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide (28):

Yield 51% ; 1H NMR (400 MHz, DMSO-d6): δ 13.00 (brs., 1H), 12.59 (br. s., 1H), 8.89 (s, 1H), 8.34 (d, = 7.6 Hz, 1H), 7.83 – 7.76 (m, 4H), 7.56 (s, 1H), 7.42 (d, = 7.9 Hz, 2H); 13C NMR (400 MHz, DMSO-d6): δ 176.8, 163.4, 144.7, 139.6, 138.2, 133.5, 129.4, 127.4, 126.4, 125.9, 125.8, 121.6, 119.7, 110.8.

[069] Example 31:

4-oxo-N-(p-tolyl)-l,4-dihydroquinoline-3-carboxamide (29):

Yield 57% ; 1H NMR (400 MHz, DMSO-d6): δ 12.94 (brs., 1H), 12.40 (s, 1H), 8.88 (s, 1H), 8.33 (d, = 7.8Hz, 1H), 7.82 – 7.80 (m, 1H), 7.76 – 7.7 (m, 1H), 7.63 (d, = 8.3 Hz, 2H), 7.53 (t, = 7.3 Hz, 1H), 7.17 (d, = 8.1 Hz, 2H), 2.29 (s, 3H); 13C NMR (100 MHz, DMSO-de): δ 176.8, 163.1, 144.5, 139.6, 136.8, 133.4, 132.8, 129.9, 126.4, 125.9, 125.7, 120.0, 119.6, 111.1, 20.9; HRMS (ESI):Calculated for Ci7H1502N2[M+H]+: 279.1128, found 279.1127.

[070] Example 32:

N-(4-ethylphenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide (30):

Yield 51% ; 1H NMR (400 MHz, DMSO-d6): δ 12.95 (br. s., 1H), 12.40 (d, = 7.8 Hz, 1H), 8.87 (d, = 6.1 Hz, 1H), 8.33 (d, = 8.1 Hz, 1H), 7.81 – 7.76 (m, 2H), 7.66 – 7.62 (m, = 8.3 Hz, 2H), 7.53 (t, 7 = 7.5 Hz, 1H), 7.22 – 7.17 (m, = 8.3 Hz, 2H), 2.58 (q, = 7.6 Hz, 2H), 1.18 (t, = 7.6 Hz, 3H); 13C NMR (400 MHz, DMSO-d6): δ 181.5, 167.8, 149.3, 144.3, 144.0, 141.7, 138.2, 133.4, 131.1, 130.7, 130.5, 124.8, 124.4, 115.9, 32.8, 20.9.

[071] Example 33:

4-Oxo-N-(4-propylphenyl)-l,4-dihydroquinoline-3-carboxamide (31):

Yield 51%; 1H NMR (500 MHz, DMSO-d6): δ12.93 (brs, 1H), 12.40 (s, 1H), 8.87 (s, 1H), 8.36 – 8.29 (m, 1H), 7.86 – 7.78 (m, 1H), 7.75 (d, J= 7.9 Hz, 1H), 7.68 – 7.61 (m, J= 8.2 Hz, 2H), 7.54 (t, J= 7.6 Hz, 1H), 7.22 – 7.14 (m, J= 8.2 Hz, 2H), 2.55 – 2.51 (m, 2H), 1.64 – 1.53 (m, 2H), 0.90 (t, J= 7.3 Hz, 3H); 13C NMR (500 MHz, DMSO-d6): 176.8, 163.1, 144.5, 139.6, 137.6, 137.0, 133.5, 129.3, 126.4, 125.9, 125.7, 120.0, 119.7, 111.1, 37.2, 24.6, 14.1.

[072] Example 34:

N-(4-isopropylphenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide (32):

Yield 46% ; 1H NMR (500 MHz, DMSO-d6): δ 12.93 (br. s., 1H), 12.40 (br. s., 1H), 8.89 – 8.86 (m, 1H), 8.33(d, = 7.6 Hz, 1H), 7.81 – 7.50 (m, 5H), 7.25 – 7.21 (m, 2H), 2.90-2.83 (m, 1H), 1.22-1. l l(m, 6H); 13C NMR (100 MHz, DMSO-d6): δ 176.8, 163.1, 144.5, 143.9, 139.6, 137.1, 133.4, 127.2, 126.4, 125.9, 125.7, 120.1, 119.6, 111.1, 33.4, 24.4.

[073] Example 35:

4-oxo-N-(4-(trifluoromethoxy)phenyl)-l,4-dihydroquinoline-3-carboxamide(33):

Yield 57% ; 1H NMR (400 MHz, DMSO-d6): δ 12.98 (br. s., 1H), 12.63 (s, 1H), 8.88 (d, = 4.9 Hz, 1H), 8.32 (d, = 7.8 Hz, 1H), 7.89 – 7.83 (m, = 8.8 Hz, 2H), 7.79 (d, = 7.6 Hz, 1H), 7.77 – 7.73 (m, 1H), 7.53 (t, J = 7.5 Hz, 1H), 7.40 – 7.34 (m, = 8.6 Hz, 2H); 13C NMR (100 MHz, DMSO-d6): δ 176.8, 163.5, 144.7, 144.0, 139.5, 138.5, 133.5, 126.3, 125.9, 125.8, 122.3, 121.4, 119.7, 110.7.

[074] Example 36:

N-(2-chloro-5-methoxyphenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide(34):

Yield 54% ; XH NMR (400 MHz, DMSO-d6): δ 12.98 (br. s., 1H), 12.49 (s, 1H), 8.88 (s, 1H), 8.33 (d, = 7.8 Hz, 1H), 7.83 – 7.75 (m, 1H), 7.56-7.48 (m, 3H), 7.27 – 7.21 (m, 1H), 6.67 (d, = 7.8 Hz, 1H), 3.77 (s, 3H); 13C NMR (400 MHz, DMSO-d6): δ 176.8, 163.4, 160.2, 144.7, 140.4, 139.6, 133.5, 130.3, 126.4, 125.9, 125.8, 119.7, 112.3, 111.0, 109.5, 105.7, 55.5.

[075] Example 37:

N-(2-ethylphenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide(35):

Yield 58% ; 1H NMR (400 MHz, DMSO-d6): δ 12.94 (br. s., 1H), 12.37 (s, 1H), 8.90 (s, 1H), 8.36 (dd, = 8.1, 1.4 Hz, 2H), 8.32 (dd, = 8.1, 1.4 Hz, 2H), 7.82 – 7.74 (m, 1H), 7.53- 7.19 (m, 3H), 7.15 – 7.06(m, 1H), 2.79 (q, = 7.3 Hz, 2H), 1.26 (t, = 7.5 Hz, 3H); 293 (M+H)+.

[076] Example 38:

N-(2-bromophenyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide(36):

Yield 47% ; 1H NMR (200 MHz, DMSO-d6): δ 12.98 (br. s., 1H), 12.69 (s, 1H), 8.90 (d, = 5.9 Hz, 1H), 8.54 (dd, 7 = 1.4, 8.3 Hz, 1H), 8.34 (d, = 7.6 Hz, 1H), 7.86 – 7.67 (m, 3H), 7.57 – 7.49 (m, 1H), 7.40 (t, = 7.2 Hz, 1H), 7.10 – 7.05 (m, 1H); 13C NMR (100 MHz, DMSO-de): δ 176.7, 163.7, 145.0, 139.5, 137.7, 133.5, 133.1, 128.6, 126.4, 126.0, 125.8, 125.3, 122.9, 119.7, 113.4, 110.8.

[077] Example 39:

N-benzyl-4-oxo-l,4-dihydroquinoline-3-carboxamide(37):

Yield 58% ; 1H NMR (400 MHz, CD3OD-d6): δ 8.82 (s, 1 H), 8.35 (d, = 8.1 Hz, 1 H), 7.79 – 7.77 (m, 1 H), 7.65 (d, = 8.3 Hz, 1 H), 7.52 (t, = 7.6 Hz, 1 H), 7.42 – 7.34 (m, 4 H), 7.31 – 7.26 (m, 1 H), 4.67 (s, 2 H); 13C NMR (400 MHz, DMSO-d6): δ 176.6, 165.0, 144.2, 140.0, 139.5, 133.2, 128.9, 128.7, 127.8, 127.3, 126.6, 125.9, 125.4, 119.5, 111.2, 42.6.

[078] ] Example 40:

N-(4-methoxybenzyl)-4-oxo-l,4-dihydroquinoline-3-carboxamide(38):

Yield 56% ; 1H NMR (400 MHz, DMSO-d6): δ 12.73 (br. s., 1H), 10.35 (t, = 5.3 Hz, 1H), 8.78 (d, = 6.1 Hz, 1H), 8.24 (d, = 8.1 Hz, 1H), 7.76 (d, = 7.1 Hz, 1H), 7.73 -7.68 (m, 1H), 7.48 (t, = 7.5 Hz, 1H), 7.28 (d, = 8.3 Hz, 2H), 6.91 (d, = 8.1 Hz, 2H), 4.49 (d, = 5.6 Hz, 2H), 3.74 (s, 3H); 13C NMR (100 MHz, DMSO-d6): δ 176.6, 164.8, 158.8, 144.1, 139.5, 133.1, 131.9, 129.2, 126.6, 125.8, 125.4, 119.5, 114.3, 111.3, 55.5, 42.0.

[079] Example 41:

N,N-dibenzyl-4-oxo-l,4-dihydroquinoline-3-carboxamide(39):

Yield 43% ; 1H NMR (400 MHz, DMSO-d6): δ 12.21 (br. s., 1H), 8.27 (d, = 4.9 Hz, 1H), 8.21 (d, = 7.6 Hz, 1H), 7.49 – 7.41 (m, 2H), 7.41 – 7.35 (m, 3H), 7.33 – 7.20 (m, 5H), 7.20 – 7.11 (m, 7 = 7.1 Hz, 2H), 4.59 (br. s., 2H), 4.42 (s, 2H).

[080] Example 42:

4-oxo-N-propyl-l,4-dihydroquinoline-3-carboxamide(40):

Yield 47% ;1H NMR (400 MHz, DMSO-d6): δ 12.7 (br.s., 1H)10.05 (t, = 5.5 Hz, 1H), 8.74 (s, 1H), 8.26 (d, = 8.1 Hz, 1H), 7.83 – 7.66 (m, 2H), 7.52 – 7.44 (m, 1H), 3.33 – 3.22 (m, 2H), 1.61 – 1.49 (m, 2H), 0.93 (t, = 7.5 Hz, 3H); 13C NMR (100 MHz, DMSO-de): δ 176.6, 164.8, 143.9, 139.5, 133.1, 126.6, 125.9, 125.3, 119.4, 111.4, 39.3, 23.1, 12.0

[081] Example 43:

N-hexyl-4-oxo-l,4-dihydroquinoline-3-carboxamide(41):

Yield 51% ;1H NMR (400 MHz, DMSO-d6): δ 12.68 (m, 1H), 10.02 (t, = 5.5 Hz, 1H), 8.73 (d, = 6.1 Hz, 1H), 8.27 – 8.25 (m, 1H), 7.77 – 7.67 (m, 2H), 7.47 (t, = 7.5 Hz, 1H), 3.33 – 3.29 (m, 2H), 1.56 – 1.45 (m, 2H), 1.34 – 1.25 (m, 6H), 0.88 – 0.82 (m, 3H); 13C NMR (100 MHz, DMSO-d6): δ 176.6, 164.8, 143.9, 139.5, 133.1, 126.6, 125.9, 125.3, 119.4, 111.4, 38.7, 31.5, 29.8, 26.7, 22.5, 14.4.

[082] Example 44:

Methyl (4-oxo-l,4-dihydroquinoline-3-carbonyl)-L-alaninate(42):

Yield 38% ; 1H NMR (400 MHz, CD3OD): δ 8.74 (s, 1H), 8.47 – 8.29 (m, 1H), 7.86 -7.76 (m, 1H), 7.64 (d, = 8.3 Hz, 1H), 7.58 – 7.44 (m, 1H), 4.69 (d, = 7.3 Hz, 1H), 3.79 (s, 3H), 1.55 (d, = 7.3 Hz, 3H); 13C NMR (100 MHz, CD3OD): δ 177.3, 173.3, 165.5, 143.6, 139.2, 132.9, 126.3, 125.4, 125.2, 118.5, 110.3, 51.5, 47.0, 17.0.

[083] Example 45:

7-chloro-4-oxo-N-phenyl-l,4-dihydroquinoline-3-carboxamide(43):

Yield 48% ; IR Omax(film): 2920, 2868, 1661, 1601 cm” 1; 1H NMR (400 MHz, DMSO-de): δ 12.91 (br. s., 1H), 12.30 (s, 1H), 8.90 (s, 1H), 8.29 (d, = 8.8 Hz, 1H), 7.80 -7.67 (m, 3H), 7.58 – 7.51 (m, 1H), 7.36 (t, = 7.7 Hz, 2H), 7.09 (t, = 7.3 Hz, 1H); 13C NMR (100 MHz, DMSO-d6): δ 176.3, 162.9, 145.4, 140.3, 139.2, 138.0, 129.5, 128.2, 126.1, 125.1, 123.9, 120.1, 118.8, 111.6.

[084] Example 46:

6-chloro-4-oxo-N-phenyl-l,4-dihydroquinoline-3-carboxamide(44):

Yield 52% ; 1H NMR (400 MHz, DMSO-d6): δ 13.05 (brs, 1H), 12.27 (s, 1H), 8.88 (s, 1H), 8.21 (d, = 2.2 Hz, 1H), 7.86 – 7.67 (m, 4H), 7.36 (t, = 7.8 Hz, 2H), 7.16 – 7.04 (m, 1H); 13C NMR (100 MHz, DMSO-d6): δ 175.6, 162.9, 144.9, 139.1, 138.2, 133.5, 130.4, 129.5, 127.5, 124.9, 123.9, 122.0, 120.1, 111.4.

[085] Example 47:

l-benzyl-4-oxo-N-phenyl-l,4-dihydroquinoline-3-carboxamide(45)

Yield 55% ; 1H NMR (400 MHz, DMSO-d6): δ 12.30 (s, 1H), 9.05 (s, 1H), 8.60 (dd, = 1.7, 8.1 Hz, 1H), 7.82 (d, = 7.8 Hz, 2H), 7.69 – 7.62 (m, 1H), 7.55 – 7.45 (m, 2H), 7.43 – 7.34 (m, 5H), 7.24 – 7.18 (m, 2H), 7.17 – 7.10 (m, 1H), 5.53 (s, 2H); 13C NMR (100 MHz, DMSO-d6): δ 176.9, 162.9, 148.7, 139.3, 138.7, 134.1, 133.1, 129.4, 128.9, 128.7, 128.0, 127.4, 126.2, 125.5, 123.9, 120.5, 116.9, 112.3, 57.9; HRMS (ESI): Calculated for C23H1802N2Na [M+Na]+: 377.1260, found 377.1259; MS: 355 (M+H)+.

[086] Advantages of invention:

1. Cost-effective process for synthesis.

2. Carried out at environmentally benign conditions.

3. Short synthetic route.

4. Useful for making several related compounds of medicinal

 

Image result for REDDY SRINIVASA DUMBALA

DR SRINIVASA REDDY recieving NASI – Reliance Industries Platinum Jubilee Award (2015) for Application Oriented Innovations in Physical Sciences.

 

Image result for REDDY SRINIVASA DUMBALA

MYSELF WITH HIM

 

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From left to right: Dr. D. Srinivasa Reddy, Shri Y. S. Chowdary, Dr. Harsh Vardhan, Dr. Girish Sahni

  • Dr D. Srinivasa Reddy receiving the prestigious “SHANTI SWARUP BHATNAGAR” award at the occasion of the 75th Foundation day of CSIR.

Shanti Swarup Bhatnagar awardees with the honorable Prime Minister of India

Image result for REDDY SRINIVASA NCL

NCL PUNE

DSR Group

//////////WO-2016181414, WO 2016181414,  IVACAFTOR, new patent, COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH,  Anusandhan Bhawan, Rafi Marg New Delhi, INDIA, CSIR, Dr. D. Srinivasa Reddy

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QbD in Pharma Development World Congress 2017, SelectBio, 20-21 April, 2017, Radisson Hyderabad HITEC City, India

 CONFERENCE, QbD  Comments Off on QbD in Pharma Development World Congress 2017, SelectBio, 20-21 April, 2017, Radisson Hyderabad HITEC City, India
Oct 212016
 

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http://selectbiosciences.com/images/DEL_QBD_20Oct.html

QbD in Pharma Development World Congress 2017 Registration

3 for 2 Offer

SELECTBIO are offering 3 for the price of 2 on all delegate passes. To take advantage of this offer contact us by email, phone or click the Contact Us button below. Looking for more than 3 passes? Contact us for more information on our special rates for large groups.

Radisson Hyderabad HITEC City

Radisson Hyderabad HITEC City

Flights

To find low cost flights, try the following websites:

Flightchecker
Travelsupermarket
Kayak

The refined Radisson Hyderabad Hitec City features the prompt services, such as a concierge, and comfortable, air-conditioned rooms you need for a satisfying visit. You can stay fit with laps in the swimming pool and fitness centre, or relax in your suite with 24-hour room service and free Wi-Fi access. The aminities include Satellite TV, Work desk, Wi-Fi access, Tea and coffeemaker, Bottles of mineral water, Large bathrooms with separate rain showers, Large wardrobe, Mini barWrap up a day of meetings with authentic Indian cuisine at Cascade or exotic Asian specialties at The Oriental Blossom. Treat your colleagues to drinks at Zyng lounge bar, or if the weather is nice, gather outside at Poolside Grill for a barbecued meal.
A business centre is also available to help you complete work while staying at this Hitec City hotel in the heart of Gachibowli, a new-age IT suburb of Hyderabad, near the Hyderabad International Convention Centre.
SELECTBIO has negotiated special rates (see below) to include buffet breakfast, and Wi-Fi. Standard Room Single/Double – INR 4500/5000+Tax
To make your reservation at these discounted rates please contact Sakshi Modgil at s.modgil@selectbio.com. We recommend early booking to avoid disappointment.

Sakshi Modgil's Profile PhotoSAKSHI MODGIL

Visa Requirements
International visitors travelling from outside India will require a Business visa.
PLEASE NOTE, THIS EVENT IS NOT ASSOCIATED WITH THE INDIAN GOVERNMENT, THEREFORE CONFERENCE VISA IS NOT APPLICABLE
International visitors will require an invitation letter to obtain their Business visa. We will only provide invitation letters to customers that are fully registered for the event. In the event of an unsuccessful visa application we will refund the full delegate fee paid.
http://selectbiosciences.com/media/VISA_Invitation_Letter_Requirements.pdf

Visa Invitation Requirement
Please ensure that the above form is duly complete, as it will expedite the preparation of an invitation letter. Also mention clearly, to whom the invitation letter should be addressed as per the requirement of the country of origin.
For more information on Indian visa’s applications for International visitors, please contact your local Indian embassy.
Please plan sufficiently in advance because processing of Indian Visa Application may take 4-6 weeks.

Copyright © 2016 SELECTBIO, All rights reserved.

This email was sent from SELECTBIO Ltd to amcrasto@gmail.com.

SELECTBIO Ltd, Woodview, Bull Lane, Sudbury, CO10 0FD, United Kingdom.

//////////QbD,  Pharma Development,  World Congress,  2017, SelectBio, Radisson Hyderabad HITEC City, India

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Register Today for the ACS Symposium in India on Recent Advances in Drug Development, 11-12 November 2016 in Hyderabad, India

 CONFERENCE  Comments Off on Register Today for the ACS Symposium in India on Recent Advances in Drug Development, 11-12 November 2016 in Hyderabad, India
Oct 142016
 

acs

cas

Inaugural ACS Industry Symposium, 11-12 November 2016 in Hyderabad, India

Recent Advances in Drug Development

Register Today for the ACS Symposium in India on Recent Advances in Drug Development

To view this email as a web page, go here.

Register now for the inaugural ACS Industry Symposium, 11-12 November 2016 in Hyderabad, India. Be sure to secure your seat today as rates will increase on 27 October!

http://acssymposium.org.in/
The theme of the Symposium is Recent Advances in Drug Development. The event will feature lectures by the world’s leading researchers and experts in the pharma industry, including:

  • Dr. Peter Senter of Seattle Genetics
  • Dr. Jagath Reddy Junutula of Cellerant Therapeutics, Inc.
  • Dr. Ming-Wei Wang of the Shanghai Institute of Materia Medica, Chinese Academy of Sciences

This is an exclusive event being organized in partnership with Dr. Reddy’s Laboratories for pharma professionals throughout India. Space is limited so register today!

Please visit our website to learn more about the speakers and the program.

Register today to ensure your access to the ACS Industry Symposium. We look forward to seeing you in Hyderabad in November.

CAS
2540 Olentangy River Rd Columbus, OH 43202 US

cas

http://acssymposium.org.in/

/////// ACS Symposium, Recent Advances in Drug Development, 11-12 November 2016, Hyderabad, India, dr reddys, cas

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11th Pharmacovigilance 2016, 1st Dec 2016, Kohinoor Continental Hotel, Mumbai, India

 CONFERENCE, Uncategorized  Comments Off on 11th Pharmacovigilance 2016, 1st Dec 2016, Kohinoor Continental Hotel, Mumbai, India
Oct 052016
 

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11th Pharmacovigilance 2016

“Ensuring safer drugs to market by analyzing latest developments in pharmacovigilance, drug safety and risk management”

1st December 2016, Kohinoor Continental Hotel, Mumbai, India

After the successful journey of a series of 10 Pharmacovigilance conferences, Virtue Insight is proud to announce its 11th Pharmacovigilance 2016 in India. It is our great pleasure to invite you to the 11th Pharmacovigilance 2016, in Mumbai – India on 1st of December 2016. We have a wide range of scientific topics with something for everyone.

The past is reflected in a session about Indian traditional medicine and the future is discussed under Big Data analytics and in the research of our young scientists. However, we must live and act in the present and debate pressing challenges that face us today in pharmacovigilance (PV). The rates for medication errors are too high. We still struggle to communicate risk well. With the welcome drive towards transparency and respecting human rights, legal and ethical issues in PV have come to the fore. Society’s research enterprise as a whole needs to become far more aware of the commercial reality that PV underpins safety, with its intimate links to innovation, so that safety and must be intrinsically built into successful development and marketing. With governments round the world struggling to curb healthcare costs, the importance of integrating PV into National Health Programmes has never been more important.

It gives me great pleasure in welcoming all of you to the virtue insight’s 11th Pharmacovigilance 2016. I wish and pray that all our efforts will be beneficial to our industries and to our country at large.

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pic KANCHI SHAH, VIRTUEINSIGHT

 

KEY SPEAKERS INCLUDE

JEAN CHRISTOPHE DELUMEAU, Head of Pharmacovigilance Asia-Pacific, Bayer HealthCare (Singapore)

Jean-Christophe Delumeau

 

JESSICA THONGCHAREN, Associate Director Pharmacovigilance, Takeda Pharmaceuticals (Singapore)

 Jessica Thongcharen

ARUN BHATT, Consultant – Clinical Research & Development
V. KALAISELVAN, Principal Scientific Officer, Indian Pharmacopoeia Commission, Ministry of Health & Family Welfare, Govt. of India
SUDHIR PAWAR, Coordinator – ADR monitoring Center at LTMMC & GH, Under Pharmacovigilance Programme Of India (PvPI),Indian Pharmacopoeia Commission
ARUN BHATT, Consultant – Clinical Research & Development
BHASWAT CHAKRABORTY, Senior VP & Chair, Research and Development Core Committee, Cadila
SUTAPA B NEOGI, Additional Professor, Indian Institute of Public Health
DEEPTI SANGHAVI, Assistant Manager – Medical Writing, Tata Consultancy Services
JAMAL BAIG, Country Head – Pharmacovigilance, Merck
SIDDHARTH DESHPANDE, Assistant Professor Department of Clinical Pharmacology, KEM Hospital
ABHAY CHIMANKAR, Head, Global Drug Safety, Cipla
SANDESH SAWANT, Head, Clinical Operations (India and EM), Wockhardt
ABHAY PHANSALKAR, Head Clinical Trials, Cipla
GURPREET SINGH, Head Vendor Management, Drug Safety & Epidemiology, Novartis
MILIND ANTANI, Partner In-Charge – Pharma LifeSciences, Nishith Desai Associates
VARSHA NARAYANAN, Head Medical Affairs, Wockhardt
POOJA JADHAV, Manager, Sun Pharmaceuticals
GODHULI CHATTERJEE, Senior Medical Advisor and Clinical Safety Officer, Sanofi-aventis

Plus Many More..

PEOPLE YOU GET TO MEET

Vice Presidents, Directors, CRO’s, Heads and Managers of:
Pharmacovigilance Strategy, Drug Safety/Risk Management, Information and Clinical Data Management, Clinical Research, Research & Development, Product Safety/Assurance Assessment, Patient Safety & Outcomes Research & Data Analysis, Epidemiology project management, Regulatory Affairs and Compliance, Sales & Marketing, Biotech manufacturers

FROM VARIOUS

Pharmaceutical organizations, Generic pharmaceutical companies, Contract research organizations, Patient recruitment companies, Government- Department of health, Non-profit organizations/ Association, Consultants
This event also serves as a platform for networking opportunities in the relevant field , wherein you get to meet and  broaden  your  contacts to develop your business. We also have sponsorship opportunities available for the event which gives you an opportunity to speak/exhibit and create brand awareness. Or you could even attend the event as a delegate and get a better insight of the updates and  the increasing challenges in the industry . So hurry now and be a part of this massive event.

 

 

GLIMPSES OF MY( DR ANTHONY) INTERACTION

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with Fen Castro of VirtueInsight, Director , and his team , , —thanks for inviting me to 9th Biosimilars Congregation 2016., Lalit hotel, Mumbai, India, 22nd Sept 2016 — with Fen Castro, Kanchi Shahand Virtue Insight at The Lalit Hotel.

 

 

CONFERENCE BOOKING DETAILS

Online Registration http://www.bookmytrainings.com/all-courses/professional-events/event/44991-11th-pharmacovigilance-2016
Early Bird Discount Price – 1 Delegate Pass (INR 6,000 + Tax (15%) – Book and Pay before 17th October 2016 to avail this price
Standard Price (From 18th October 2016) – 1  Delegate Pass – (INR 7,000 + Tax (15%)
Group Discounts (Applicable for 3 or 4) – 1 Delegate Pass  – (INR 6,500 + Tax (15%)
Group Discounts (Applicable for 5 or more) – 1 Delegate Pass  – (INR 6,000 + Tax (15%)
Conference Sponsor & Exhibition Stall – Should you wish to Sponsor, Exhibition Stall (Booth) or a paid Speaker Slot, you can simply call or email your interest and queries to TEL: +91 44 64614333, or sponsor@virtueinsight.com

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REGISTRATION PROCESS

In order to register simply email the below mentioned details to delegate@virtueinsight.com

  • Company Name & Address
  • Attendee Name/Names
  • Job Title
  • Contact Number

We also have some sponsorship opportunities available for the event, which gives you an opportunity to speak/exhibit, and create brand awareness. In addition, the networking opportunities in focused and relevant industry gathering provide the personal contact necessary for business development efforts.

In case you or any of your colleagues might be interested in participating in the same, please let us know and we will be happy to call you and help you with the registration.

 

SEE BROCHURE

Image result for waitALLOW BROCHURE TO LOAD

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Thank you for your time and consideration.

Fen Castro

Head – Productions

Virtue Insight

Image result for FEN CASTRO

Tel (India) –       + 91 44 64614333

Mobile (India) –  + 91 9003 26 0693

Tel (UK) –          + 44 2036120886

 

 

 

////////////11th Pharmacovigilance,  2016, 1st Dec,  2016, Kohinoor Continental Hotel, Mumbai, India, Conference, fen castro

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Dr. D. Srinivasa Reddy of NCL receives the Shanti Swarup Bhatnagar Prize New Delhi, India

 Uncategorized  Comments Off on Dr. D. Srinivasa Reddy of NCL receives the Shanti Swarup Bhatnagar Prize New Delhi, India
Sep 292016
 

 

Indian flag

dsreddy-receiving-ssb-award

ssb-awardees-with-pm

Dr. D. Srinivasa Reddy of NCL receives the Shanti Swarup Bhatnagar Prize New Delhi, India

Dr. D. Srinivasa Reddy
Senior Scientist
Organic Chemistry Division
National Chemical Laboratory
PUNE, INDIALINKS
 

 NCL PUNE INDIA

 WEBSITE–http://www.ncl-india.org/

Dr. Srinivasa Reddy of CSIR-NCL bags the prestigious Shanti Swarup Bhatnagar Prize

The award comprises a citation, a plaque, a cash prize of Rs 5 lakh

dr

The Shanti Swarup Bhatnagar Prize for the year 2015 in chemical sciences has been awarded to Dr. D. Srinivasa Reddy of CSIR-National Chemical Laboratory (CSIR-NCL), Pune for his outstanding contributions to the area of total synthesis of natural products and medicinal chemistry.
This is a most prestigious award given to the scientists under 45 years of age and who have demonstrated exceptional potential in Science and Technology. The award derives its value from its rich legacy of those who won this award before and added enormous value to Indian Science.
Dr. Reddy will be bestowed with the award at a formal function, which shall be presided over by the honourable Prime Minister. The award, named after the founder director general of Council of Scientific & Industrial Research (CSIR), Dr. Shanti Swarup Bhatnagar, comprises a citation, a plaque, a cash prize of Rs 5 lakh.
Dr. Reddy’s research group current interests are in the field of total synthesis and drug discovery by applying medicinal chemistry. He has also been involved in the synthesis of the agrochemicals like small molecules for crop protection. The total synthesis of more than twenty natural products has been achieved in his lab including a sex pheromone that attracts the mealy bugs and has potential use in the crop protection. On the medicinal chemistry front significant progress has been made by his group using a new concept called “Silicon-switch approach” towards central nervous system drugs. Identification of New Chemical Entities for the potential treatment of diabetes and infectious diseases is being done in collaboration with industry partners.
His efforts are evidenced by 65 publications and 30 patents. He has recently received the NASI-Reliance industries platinum jubilee award-2015 for application oriented innovations and the CRSI bronze medal. In addition, he is also the recipient of Central Drug Research Institute award for excellence in the drug research in chemical sciences and scientist of the year award by the NCL Research Foundation in the year 2013. Dr. Reddy had worked with pharmaceutical companies for seven years before joining CSIR-NCL in 2010.

His team

 

//////////Dr. D. Srinivasa Reddy,  NCL, Shanti Swarup Bhatnagar Prize,  PM, Narendra Modi,

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CHIRAL INDIA 2016, 5th International Conference & Exhibition Nov 8-9 2016, Holiday Inn, Mumbai, India

 CONFERENCE  Comments Off on CHIRAL INDIA 2016, 5th International Conference & Exhibition Nov 8-9 2016, Holiday Inn, Mumbai, India
Sep 072016
 

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India's only conference focusing on new chiral technologies for pharmaceutical fine chemicals. The event is a unique platform to learn about recent advances in chiral chemistry, technology and application.

Chiral India series which began in 2012 has now grown into a major must-attend event for the Pharmaceutical industry. This platform is the most popular chiral technology platform bringing together the top experts from China, Canada, USA, Japan, India and other countries to present the latest developments in chiral drug developments and brainstorm with leading R&D personnel from Indian pharmaceutical industry.

The fifth edition of Chiral India to be held on 8-9 November 2016, at Holiday Inn (Mumbai), follows the success of previous four annual editions (2012, 2013, 2014 and 2015) and is now an event awaited by R&D professionals across the industry.

International panel of Chiral experts will address on key Themes
  • Asymmetric hydrogenations: New directions
  • Chiral switches: Development of single enantiomer drugs
  • Chiral tool kit in new drug development
  • Organo molecular catalysts
  • Enzymatic processes for new chiral drug synthesis
  • Chiral chemistry in natural product synthesis
  • Chiral catalysis: An overview of recent advances
  • Chiral drugs: New regulatory directions
  • Chiral separation technologies
  • Flow reactions for chiral drug development

R  Rajagopal

+9198211 28341

rraj@chemicalweekly.com

kiran@chemicalweekly.com

Dr. R. Rajagopal B-602, Godrej Coliseum Tel: +91 22 24044477
Editorial Advisor K.J. Somaiya Hospital Road Fax: +91 22 24044450
Chemical Weekly Sion (East) Mumbai 400 022 www.chemicalweekly.com

DOWNLOAD BROCHURE…..

Please use http://www.chiralindia.com/Brochure.pdf link to download the Brochure.

Our website URL is www.chiralindia.com

 

Oganised By

 

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SCROLL USING MOUSE TO VIEW 5 PAGES

////////CHIRAL INDIA 2016, 5th International Conference, Exhibition,  Nov 8-9,  2016, Holiday Inn, Mumbai, India

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Training Course РIN SILICO DRUG DISCOVERY & DESIGNING: INSIGHTS OF PROTEIN-LIGAND INTERACTIONS. Oct 01, 2016 at Le M̩ridien Bangalore Hotel in Bengaluru, India.

 CONFERENCE  Comments Off on Training Course – IN SILICO DRUG DISCOVERY & DESIGNING: INSIGHTS OF PROTEIN-LIGAND INTERACTIONS. Oct 01, 2016 at Le Méridien Bangalore Hotel in Bengaluru, India.
Aug 222016
 

 

Training Course – IN SILICO DRUG DISCOVERY & DESIGNING: INSIGHTS OF PROTEIN-LIGAND INTERACTIONS. Oct 01, 2016  at Le Méridien Bangalore Hotel in Bengaluru, India.

https://selectbiosciences.com/trainingCoursesID.aspx?tc=DDD16&pid=4820&conf=DDI16&se=india

http://selectbiosciences.com/conferences/index.aspx?conf=DDI16&se=india

http://selectbiosciences.com/conferences/venue.aspx?pid=4817&conf=DDI16&se=india

Dear Colleague,

SELECTBIO would like to remind you about its Training Course – IN SILICO DRUG DISCOVERY & DESIGNING: INSIGHTS OF PROTEIN-LIGAND INTERACTIONS. This is scheduled to be held on October 01, 2016 from 9:00am to 5:00pm at Le Méridien Bangalore Hotel in Bengaluru, India. This course will be held in conjunction with our 4th International Conference “Drug Discovery India 2016“. Attend the Training Course and the Conference andSave 10% against the regular registration charges.

PROFILE OF ATTENDEES
With basic knowledge in Life Science and Drug Design that would like to receive a comprehensive overview or refresher on the Drug Discovery Technology the target audience comprises:
• Student & Faculty: Bachelor, Masters, PhD, students as well as Faculty and Professors from Microbiology, Biochemistry, Biotechnology, Immunology, Pharmacy, Pharmaceutical Chemistry, Biomedical Technology, Genetics, Bioinformatics, Plant Science and Life Sciences.
• Professionals: Biotechnology, Bioinformatics and Pharmaceutical scientists from industry, academia and regulatory agencies.
Hands-on exercises will be performed individually using Software tools (no prior experience required).

COURSE CONTENTS

• Introduction of Drug Designing
• Science involved in Disease Target Identification
• Virtual Screening
Practical application will be done on 5 molecules and the software on which DEMONSTRATION & TRAINING will be given
• In-Silico Generation of Ligands by ChemSketch
• Conversion of mol files to pdf files by Open Babel
• Protein Optimization & Energy Minimization by SPDBV
• Molecular Docking by MGL Tools | Creation of Grid Parameter & Dock Parameter Files by AutoDock Software
• Running the Algorithm by Cygwin
• Selection of Potent Inhibitors on the basis of Binding Energies and Lipinski’s Rule of 5
• Structure Analysis – Protein & Ligand complex H-bond interaction by UCSF Chimera
• Prediction of Molecular Properties- Molinspiration
• Prediction of Bioactivity- Molinspiration & ACD iLabs
• Drug Likeness – Mol Soft
• Bioavailability & ADME- ACD iLabs
• Toxicity- OSIRIS Property Explorer & ACD iLabs

For more information, or to discuss registration options, please contact me on the details given below.

Thanks and Best Regards

Sakshi Modgil
Customer Services Manager
SELECTBIO INDIA
O: +91 172 5025050
M: +91 7696125050
s.modgil@selectbio.com

Copyright © 2016 SELECTBIO, All rights reserved.

 

///////////////Training Course,  IN SILICO DRUG DISCOVERY & DESIGNING, INSIGHTS OF PROTEIN-LIGAND INTERACTIONSOct 01, 2016  at Le Méridien Bangalore Hotel,  Bengaluru, India, selectbio

 

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Flow Chemistry Symposium + Workshop on 27-28th Aug’ 2016 at IISER – PUNE, Pune, India

 SYNTHESIS  Comments Off on Flow Chemistry Symposium + Workshop on 27-28th Aug’ 2016 at IISER – PUNE, Pune, India
Aug 192016
 

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Flow Chemistry Society – India Chapter is assisting the proliferation of Process Intensification and Flow Chemistry across the country

After  an  enthusiastic  response  at the  2nd FCS-India Symposium & Workshop held at IICT-Hyderabad  in June’16  with  27companies and 115 delegates attending,  we are happy to announce :

The 3rd   2-day FLOW CHEMISTRY Symposium + DEMO Workshop is organized on 27th – 28th August 2016 at  IISER – PUNE  by Flow Chemistry Society – India Chapter (in collaboration with IISER-Pune,  NCL  & IIT-B) ,  with speakers & demonstrators from India, UK, Netherlands and Hungary.

Prof. Ashwini Kumar Nangia,  Director – CSIR-NCL has kindly consented to be the Hon. Chief Guest and inaugurate the Symposium & Workshop.

Both days have intensive interactive sessions on the theory and industrial applications of Flow Chemistry followed by  livedemonstrations  using              5 to 6 different Flow Reactor platforms –each day  from microliters to 10,000 L/day  industrial scale.

The Fees are Rs. 7,000 for Industry Delegates and Rs. 3,000 for Academic Delegates

The registration form  is BELOW

CLICK FOR REGISTRATION FORM 1-REGISTRATION FORM

contact : vk@pi-inc.co   or   msingh@cipla.com   or    rentala@inkarp.co.in 

Accomodation (optional)  : for Bookings please contact IISER-Pune Guest House directly

Mr. Charu Gurav; Mgr Guest Hse, managergh@iiserpune.ac.in   020-25908130    OR

Mr. Sreejit, Mgr-Catering, etc.    sreejit@iiserpune.ac.in    020-25908247

Tariff  per room night :  Rs. 1,500 (single occupancy) //  Rs. 2,000 (Double Occupancy)

best regards

 Vijay

                             Flow Chemistry Society – India Chapter

Vijay Kirpalani                                                                                      Manjinder Singh
President                                                                                Vice-President
email : vk@pi-inc.co                                                                         email : msingh@cipla.com

Tel: +91-9321342022                                                          Tel: +91-9321342022

CLICK FOR REGISTRATION FORM 1-REGISTRATION FORM

/////////

Day 16 of the 2016 Doodle Fruit Games! Find out more at g.co/fruit

P V SINDHU OF INDIA WINS SILVER AT RIO 2016 OLYMPICS IN BADMINTON

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Innogen summit India 2016, 18-19 Aug, Mumbai, India

 CONFERENCE  Comments Off on Innogen summit India 2016, 18-19 Aug, Mumbai, India
Aug 192016
 

 

i1Innogen summit India 2016, 18-19 Aug, Mumbai, India, HOTEL HOLIDAY INN, Mumbai International Airport,Organised by Inventicon Business Intelligence Pvt. Ltd………topic is Supergenerics, Innovation in Generics, commercialization, regulatory, other insights,

 

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Dr. Ashok Kumar, President – Centre for Research & Development, Ipca Laboratories Ltd, at Innogen summit India 2016, 18-19 Aug, Mumbai, India,, HOTEL HOLIDAY INN, Mumbai International Airport,Organised by Inventicon Business Intelligence Pvt. Ltd — with DR ASHOK KUMAR OF IPCA at Holiday Inn-Mumbai Intl Airport.

 

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PANEL DISCUSSION, Dr. Ashok Kumar, President – Centre for Research & Development, Ipca Laboratories Ltd , Dr. Nilima A. Kshirsagar, National Chair Clinical Pharmacology, ICMR Government of India, Yugal Sikri, Chairman – Pharmaceutical Management, School of Business Management, SVKM’s Narsee Monjee Institute of Management Studies — with Yugal Sikri,, Nilima A. Kshirsagarand ASHOK KUMAR OF IPCA at Holiday Inn-Mumbai Intl Airport.

ashit

Ashit sikka, Koji nakamura, Uttam kumar, allfdron TERUMO, AT Innogen summit India 2016, 18-19 Aug, Mumbai, India,, HOTEL HOLIDAY INN, Mumbai International Airport,Organised by Inventicon Business Intelligence Pvt. Ltd — with Koji nakamura of terumo, Ashit Sikka and UTTAM KUMAR OF TERUMO at Holiday Inn-Mumbai Intl Airport.

 

INNO1 INNO3

ROHAN, RIDDHI AND PALLAVI OF INVENTICON

INNO4 S2

DR NIDHI SAPKAL OF ZIMLABS

S3

ALKA LUTHRA OF LUBRIZOL

 

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DR SEEMA SINGH, VP AND HEAD,-LEGAL AND IPM, MACLOEDS PHARMA, Innogen summit India 2016, 18-19 Aug, Mumbai, India,, HOTEL HOLIDAY INN, Mumbai International Airport,Organised by Inventicon Business Intelligence Pvt. Ltd — withSeema Singh.

 

lupin cadila

standing Mr Rajeev patil, Sr VP reg affairs Lupin and Mr Sushrut kulkarni Sr VP Zydus cadila, Head, Pharma tech cemtre — with sushrut kulkarni andrajeev patil.

Thanks to

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Rohan Jagtap

Program Manager – Pharma & Lifesciences

 https://ci4.googleusercontent.com/proxy/XM6zLJNVF-KyjTdLe4_K-jsjBvWCfPVibLEfkfFi-qr6U362NxG0XVUkvsdpOUKmwJgUMkzmSETrv9F_bY4Pv0rEVxiUozAcfOcwUjawrQs2stF7iWDvdLcVkMJYElp6G8kNSGlsGwZJsFOoqQTnShF3BCHD=s0-d-e1-ft#https://docs.google.com/a/inventiconasia.com/uc?id=0BxGiCo9okSEbVlRmN0xxM1dpc1E&export=download

Inventicon Business Intelligence Pvt. Ltd.

Phone: +91 22 6511 3334 I Mob: +91 9011052025 Email: rohan.jagtap@inventiconasia.com

Times Square, Unit 1, Level 2, B Wing, Andheri Kurla Road, Andheri (E), Mumbai – 400059, MS – India.

http://inventiconasia.com/About-Us.aspxgards,

AGGENDA

////////

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