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DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Worlddrugtracker, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his PhD from ICT ,1991, Mumbai, India, in Organic chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA as ADVISOR earlier GLENMARK LS Research centre as consultant,Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Prior to joining Glenmark, he worked with major multinationals like Hoechst Marion Roussel, now sSanofi, Searle India ltd, now Rpg lifesciences, etc. he is now helping millions, has million hits on google on all organic chemistry websites. His New Drug Approvals, Green Chemistry International, Eurekamoments in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 year tenure, good knowledge of IPM, GMP, Regulatory aspects, he has several international drug patents published worldwide . He gas good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, polymorphism etc He suffered a paralytic stroke in dec 2007 and is bound to a wheelchair, this seems to have injected feul in him to help chemists around the world, he is more active than before and is pushing boundaries, he has one lakh connections on all networking sites, He makes himself available to all, contact him on +91 9323115463, [email protected]

Amidation of phenol derivatives: a direct synthesis of paracetamol (acetaminophen) from hydroquinone

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May 302014
 

Green Chem., 2014, 16,2997-3002
DOI: 10.1039/C4GC00166D, Communication
Roxan Joncour, Nicolas Duguet, Estelle Metay, Amadeo Ferreira, Marc Lemaire
Paracetamol (acetaminophen) was prepared from hydroquinone and ammonium acetate in acetic acid with 88% yield and >99% purity.
A direct synthesis of paracetamol (acetaminophen) from hydroquinone has been developed using ammonium acetate as an amidating agent. The reaction proceeds in acetic acid at elevated temperatures without any metallic catalyst. Under these conditions, paracetamol was obtained with high yield and selectivity (>95%). The reaction has also been carried out on the multi-gram scale (44 g of hydroquinone) and a potential process has been proposed based on the recycling of the solvent and by-products. This amidation protocol has also been extended to other phenol derivatives.
ANTHONY MELVIN CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

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Patient stem cells used to make ‘heart disease-on-a-chip’

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May 302014
 


Researchers use modified RNA transfection to correct genetic dysfunction in heart stem cells derived from Barth syndrome patients. The series of images show how inserting modified RNA into diseased cells causes the cells to produce functioning versions of the TAZ protein (first image: in green) that correctly localize in the mitochondria (second image: in red). When the images are merged to demonstrate this localization, green overlaps with red, giving the third image a yellow color. (Credit: Gang Wang and William Pu/Boston Children’s Hospital)

 

Harvard scientists have merged stem cell and ‘organ-on-a-chip’ technologies to grow, for the first time, functioning human heart tissue carrying an inherited cardiovascular disease. The research appears to be a big step forward for personalized medicine, as it is working proof that a chunk of tissue containing a patient’s specific genetic disorder can be replicated in the laboratory.

The work, published in Nature Medicine, is the result of a collaborative effort bringing together scientists from the Harvard Stem Cell Institute, the Wyss Institute for Biologically Inspired Engineering, Boston Children’s Hospital, the Harvard School of Engineering and Applied Sciences, and Harvard Medical School. It combines the ‘organs-on-chips’ expertise of Kevin Kit Parker, PhD, and stem cell and clinical insights by William Pu, MD.

read at

http://hsci.harvard.edu/news/patient-stem-cells-used-make-%E2%80%98heart-disease-chip%E2%80%99#.U4eNnBFG6qk.facebook

 

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Tug Of War Over Promising Cancer Drug Candidate Drug Discovery: Structure error threatens existing patent and clinical trials

 cancer  1 Response »
May 222014
 

09221-notw1-strucs

Misassigned (top) and corrected (bottom) structures of bioactive TIC10.

Tug Of War Over Promising Cancer Drug Candidate

Drug Discovery: Structure error threatens existing patent and clinical trials

A promising anticancer agent about to enter human clinical trials is on the hook because of a chemical structure error discovered by scientists at Scripps Research Institute California. The patented compound, known as TIC10 or ONC201, is owned by the biotech firm Oncoceutics. However, Scripps has applied for a patent on the corrected structure and has licensed it exclusively to another company, Sorrento Therapeutics.

The reanalysis and relicensing could lead to an unprecedented legal case—the first in which a structural reassignment puts in jeopardy a patent and clinical trials.

Lee Schalop, Oncoceutics’ chief business officer, tells C&EN that the chemical structure is not relevant to Oncoceutics’ underlying invention. Plans for the clinical trials of TIC10 are moving forward.

 

read at

http://cen.acs.org/articles/92/web/2014/05/Tug-War-Over-Promising-Cancer.html

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1-((3-methoxyphenyl)sulfonyl)piperidine …learn spectroscopy

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May 152014
 

1-((3-methoxyphenyl)sulfonyl)piperidine (2) is a crystalline white solid

1-((3-Methoxyphenyl)sulfonyl)piperidine: Piperidine,

1-[(3-methoxyphenyl)sulfonyl]-; (2) cas no (173681-65-7)

mp 115-116 °C;

1H NMR pdf

(400 MHz, DMSO-d6, 2.50 ppm)

δ: 1.30-1.35 (m, 2 H, N(CH2CH2)2CH2),

1.47-1.52 (m, 4 H, N(CH2CH2)2CH2),

2.85 (t, J = 5.2 Hz, 4 H, N(CH2CH2)2CH2),

3.83 (s, 3 H, OMe),

7.16 (t, J = 2.1 Hz, 1 H, Ar-H),

7.25-7.30 (m, 2 H, Ar-H),

7.55 (t, J = 8.0 Hz, 1 H, Ar-H);

 

13C NMR pdf

(100 MHz, DMSO-d6, 39.5 ppm)

δ: 22.8, 24.7, 46.6, 55.6, 112.3, 118.7, 119.5, 130.5, 136.7, 159.5;

 

IR nmax (film)/cm-1 2940, 2851, 1597, 1478, 1359, 1340, 1318, 1287, 1241, 1167, 1098, 1040, 931, 856, 724, 688; (principal peaks);

HRMS (FTMS+p-NSF) found m/z 256.1002 [M+H]+, C12H18 NO3S requires m/z 256.1002.

 

Reverse phase HPLC analysis reveals purity >99% (run on an Agilent Zorbax SB-C18, 5 µm, 4.6 x 150 mm column (23 °C) at a flow rate of 1.5 mL/min of 75:25 MeCN:H2O observed at 210 nm giving a retention time of 1.95 min, 1.0 mg/mL in MeCN).

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NMR EXAMPLE

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May 152014
 

<br /><br /> Reaction Scheme: <IMG src="/images/empty.gif">Deprotection of a tert-butyldimethylsilyl ether<IMG src="/images/empty.gif">

 

1H NMR (300 MHz; (CD3)2CO)
11.76 (1 H, s, OH (naph.) [exch]),
8.74 (1 H, dd, J 8.5 and 1.0, naph.),
8.10 (1 H, d, J 9.0, naph.),
7.89 (1 H, dd, J 8.5 and 1.5, naph.),
7.86 (1 H, dd, J 6.5 and 2.0, cyclop.),
7.59 (1 H, ddd, J 8.5, 7.0 and 1.5, naph.),
7.41 (1 H, ddd, J 8.5, 7.0 and 1.0, naph.),
7.22 (1 H, d, J 9.0, naph.),
6.50 (1 H, dd, J 6.5 and 2.0, cyclop.),
6.18 (1 H, q, J 2.0, cyclop.),
5.26 (1 H, d, J 5.5, OH (cyclop.) [exch]),
4.69 (1 H, dd, J 5.5 and 2.0, cyclop.)

 

Reference s

J. H. Clark, Chem. Rev., 1980, 80, 429 doi:10.1021/cr60327a004
E. J. Corey, A. Venkateswarlu, J. Am. Chem. Soc., 1972, 94, 6190 doi:10.1021/ja00772a043
A. B. Smith, III, G. R. Ott, J. Am. Chem. Soc., 1996, 118, 3095 (TBAF/AcOH)
K. C. Nicolaou, S. E. Webber, Synthesis, 1986, 453 (HF.py) doi:10.1055/s-1986-31673
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