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, amcrasto@gmail.com

Pharmaceutical Royal International society (PRISAL), 1st Pharma conference, Bhopal, India 26 may 2019

ANTHONY CRASTO, CONFERENCE Comments Off

Apr 272019

Venue at State Animal Husbandry Training Institute , Bhopal, MP, India

We are delighted to have Dr.Anthony Melvin Crasto
Principal Scientist Glenmark Pharma as a “Guest of Honor ” at the 1st Pharma Conference on Pharmaceuticals -bench to bedside : challenges,recent initiatives and Future advancements in the Month of May 26th 2019. It will be a huge privilege to have you with us at this national conference.
#PRISAL

It is a Great honour indeed to be at Pharmaceutical Royal International society (PRISAL)
Thanks to Dr Priti Tagde for the honour and an opportunity to visit great city Bhopal MP, India for
1st Pharma Conference on Pharmaceuticals -bench to bedside : challenges,recent initiatives and Future advancements May 26th 2019. Bhopal, Mp, India

link https://www.facebook.com/Pharmaceutical-Royal-International-Society-2323710884572948/

www.prisalpharma.org

Pharmaceutical Royal International Society

DR PRITI TAGDE

+919098598114

💯 most impactful Healthcare Global leaders
Pharma Ratan Awardee
Outstanding Achievement Award

Associate Professor at Bhabha University

others……

Dr. Ranjit Barshikar , QbD international and Quality expert United Nations

Dr.Rupali Tasgaonkar
Principal Yadavrao Tasgaonkar Institute of Pharmacy

Mr. Sacheen Gandhi Co Founder FHER

Dr.Sidharth Mehan an Associate Professor ISF College of Pharmacy Moga Punjab

Dr.Narendra Joshi Senior Director Laxai Life Sciences

Dr.Murlidhar Ingle Director Adroit Pharma Pvt.Ltd

BHOPAL, MP, INDIA

Bada Talaab

Taj-ul-Masajid

Image result for bhopal

Raja Bhoj International Airport

Taj-ul-Masajid Aerial Photo

Train installation from Bhopal upper lake

FOOD IN BHOPAL

1. Jamal Bhai Tea Shop

Jamal Bhai Tea Shop

Source

Suleimani Chai is a special variety of tea that offers a fine balance of flavors, with a hint of sugar and salt. Served with a generous dollop of cream, it is sure to intrigue your taste buds and open your senses to a new day. This type of tea is offered in several parts of India, but the variety served in Bhopal is truly unique. And no better place to enjoy this tea, than Jamal Bhai Tea Shop at Itawar Chowk in Old Bhopal. You will know you have reached the right place when you see a large crowd of people sipping tea. The tea is served from a large samovar (something similar to a boiler used in the south). This slightly unusual and salty tea is certain to leave you mesmerized and wanting more.

2. Paya Soup in Chatori Gali

Paya Soup in Chatori Gali

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Chatori Gali is to Bhopal what Chandni Chowk is to Delhi, or Mohammed Ali Road is to Mumbai. If you happen to come to this food heaven, you simply cannot miss the mutton Paya soup, lamb slow-boiled in a broth all day long and delicately spiced. Quite unlike the Paya soup found in other parts of the country, the Paya soup served here is quite thick (by use of corn or wheat flour) and is less oily as well. Come sundown, the deliciously thick soup is poured into bowls, and is garnished with lamb shreds, spices and chopped coriander. It serves as a great appetizer, before you embark on a memorable gastronomic adventure in this humble gali.

3. Poha Jalebi at Kalyan Singh’s Swaad Bhandar

Poha Jalebi at Kalyan Singh's Swaad Bhandar

Source

If you are in the mood for some vegetarian goodness, the first place you should head out to is Kalyan Singh’s Swad Bhandar. Located on the east side of the Jama Masjid, off Itwara Road, it is always crowded and noisy here. Fresh, hot, moist, light and spicy Bhopali Poha garnished with a generous helping of crispy sev and served with some oh-so-yummy jalebis, it is sure to teleport you to food heaven. Poha Jalebi is the most famous breakfast that can be found all over M.P., but the best is found in Indore. These same Indoris serve this delicacy in Bhopal, making it a sumptuous and memorable breakfast that is light, enjoyable, delicious and easy on the pocket. Wash it down with a piping hot cup of Suleimani chai, and you can face all the troubles of the day head on.

4. Cycle Soupwala and Sagar Gaire Snacks

Cycle Soupwala and Sagar Gaire Snacks

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Bhopal’s famous Cycle Soupwala, located in Number 10, is a real-life rags-to-riches story. The owner of this humble eatery, so named because he sells delicious soup on a bicycle, came to this city from Nepal. He started off by selling three types of soup: tomato, sweet corn and manchow on a bicycle, to satisfy the hunger pangs of students and office-goers alike. His soup stall set him on the path to success and today he owns a chain of eateries in Bhopal, that serve everything from cold coffee to sandwiches, dosas to chole kulche. Neither his soup nor his eateries are something you should miss if you are in Bhopal, and looking for some yummy food.

5. Bade ke Kebab at Jhili Miyaan

Bade ke Kebab at Jhili Miyaan

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After a hard day’s work, if you are looking for something to set your taste buds on fire, Jhili Miyaan is the place to be. Located at the beginning of the Chatori Galli, this tiny shop sells the most amazing melt-in-your-mouth kebabs. Bade ke Kebab are essentially beef kebabs, made from minced beef, marinated all day in a spice mix. The kebabs are then rolled by hand, fried on a hot pan and stuffed inside grilled buns. The entire dish is made-to-order and is always served steaming hot served with a mix of onions, chutneys and chilies. Juicy, succulent kebabs, served with hot buns and a spicy chutney, is sure to melt away all your troubles. You can eat to your stomach’s content but never to your heart’s content!

6. Bhopali Paan

Bhopali Paan

Source

Paan is the traditional Indian way to end a meal in style. It is loved and consumed all over the country, and each region adds its own unique touch to the paan. Bhopali paan is very famous all over the country, and when you are here, this is not something you must miss. It is a pastry made from betel nut, stuffed with chuna, kattha and supari, and a generous dollop of gulkand. Paan-making is considered an art in Bhopal, and is part of the local culture. It is usually consumed as a mouth freshener though people can be found chewing paan throughout the day.

7. Shahi Tukda in Koh-e-Fiza

Shahi Tukda in Koh-e-Fiza

Source

If all the spicy food is making you nauseous and you need a refresher, Shahi Tukda is what you should have. Indulgence that is easy on the pocket, Shahi Tukda is the perfect sweet treat for you. It is made of fried bread soaked in a decadent custard, and garnished with nuts and spices. Don’t worry if things turn too sweet, that’s how it is meant to be in Bhopal. Koh-e-Fiza is the place to have this rich delicacy.

8. Kebabs at Jameel

Kebabs at Jameel

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After a hard day of shopping and doing touristy things in Old Bhopal, if you are on the hunt for some pet-pooja, head out to Jameel in Ibrahimpura. This is a busy lane in a busy area of the market housing a lot of bakeries, and the food is to die for! Rich succulent kebabs made of chicken or mutton, delicious egg curry and mutton stew ? all at a pocket-friendly price. Delicious food, fast service with affordable pricing, what else is it that you need?

9. Chaat at 6 Number Stop Hawkers Corner

Chaat_ 6 Number Stop Hawkers Corner

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If you are in the newer side of town and looking for some place to appease your taste buds, this one will not disappoint you. The Hawkers corner in 6 Number stop is sure to leave you drooling. Famous for all types of chaat like pani puri, dahi puri, bhel puri and chole tikki, and ice golas and faloodas, for those looking for something sweet, this is the most famous place to grab a quick bite. Special recommendation ? try the samosa kachori chaat. Tangy, tasty, spicy goodness that tickles your taste buds, leaving you wanting more.

10. Raju Tea Stall

Raju Tea Stall_Holdiify

Source

Also known as Fareed Bhai’s tea stall, it is hard to come across a Bhopali who has never had tea from this iconic tea stall, which is a landmark in itself. Situated in Old Bhopal near the Peer Gate area, it is the best location to have a cuppa with friends. Enjoy a steaming hot cup of Nawabi tea, which was a favorite of the royals and is famous among the locals, have some piping hot snacks, and just watch the city go by.

11. Barfi Rasmalai at Surendra Jain’s stall

Barfi Rasmalai _ Surendra Jain's stall_Holidify

Source

If you happen to be near the Jama Masjid, head over to the chowk adjacent to the masjid to taste something you have probably never tasted before ? barfi rasmalai drona. It is perhaps as whacky as it sounds, and is super-delicious. He takes a drona ( bowl made from dried leaves) , heaps up crushed ice, and then laps it up in a sweet, rich rabri, flavored syrup and rose water. Ice-cold, sweet and delicious, you would want to keep eating more of this wonderful street food. Have a bowlful as a palate refresher before you dig in through all those meat treats in Chatori Galli.

12. Manohar Dairy and Restaurant

Manohar Dairy and Restaurant_Holidify

Source

If you are in Bhopal, this is one place you absolutely must visit. A landmark in itself, Manohar Dairy and Restaurant has been standing tall since 1970 in Hamidia Road, and has been a witness to the growth of this buzzing city. As they keep adding in new restaurants and introducing a whole new array of dishes, the yesteryear charm is still intact. Two of their must-try dishes are the dahi puri and the chhole puri/kulche ? relished and recommended by generations of Bhopalis for years together.

13. Haji Lassiwala

Haji Lassiwala_Holidify

Source

A rich, decadent shake made from milk and cream, served with a generous helping of glassy, sugary, sweet noodles ? that is falooda for you. To make it even more irresistible, several flavoring syrups, dried fruits and nuts are added. It is a uniquely Indian dish and it is best had after a long post-dinner walk. And the best place to have it is Haji Lassiwala at Itwara Chowk in Old Bhopal. Locals say it is the world’s best falooda, and if a Bhopali says that, it might just be true!

14. Al Beik

This food joint has multiple franchises across Bhopal. An economical substitute to KFC, Al Beik serves mouth-watering Chicken Burgers, Nuggets, Chicken Strips making it a must-visit place for all chicken lovers.

Al Beik

Source

CREDIT

https://www.holidify.com/pages/bhopal-street-food-1506.html

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Basic Anion-Exchange Resin-Catalyzed Aldol Condensation of Aromatic Ketones with Aldehydes in Continuous Flow

organic chemistry, PROCESS Comments Off

Apr 262019

A general method for the aldol condensation of aromatic ketones with aldehydes was developed under continuous-flow conditions using a commercially available, strongly basic anion-exchange resin (A26) as catalyst. This procedure, in addition to exhibiting a wide substrate scope, promoted carbon–carbon bond formation under mild conditions using a quasi-stoichiometric ratio of starting reagents with good to excellent yields, thereby forming a limited amount of waste and allowing the process to be applied to sequential-flow systems. A proof of concept was developed in the first fully heterogeneously catalyzed two-step flow synthesis of donepezil, which is a blockbuster commercial anti-Alzheimer’s drug.

Basic Anion-Exchange Resin-Catalyzed Aldol Condensation of Aromatic Ketones with Aldehydes in Continuous Flow

Benjamin Laroche^†, Yuki Saito^†, Haruro Ishitani^‡, and Shu̅ Kobayashi*^†^‡

^†Department of Chemistry, School of Science, and ^‡Green & Sustainable Chemistry Social Cooperation Laboratory, Graduate School of Science, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/acs.oprd.9b00048

*E-mail: shu_kobayashi@chem.s.u-tokyo.ac.jp.

https://pubs.acs.org/doi/10.1021/acs.oprd.9b00048

////////donepezil

Design, synthesis and antimicrobial activity of usnic acid derivatives

Uncategorized Comments Off

Feb 012019

Design, synthesis and antimicrobial activity of usnic acid derivatives

Victor Kartsev,^a Boris Lichitsky,^b Athina Geronikaki,*^c Anthi Petrou,^c Marija Smiljkovic,^d Marina Kostic,^d Oliver Radanovic^e and Marina Soković^d

Author affiliations

*Corresponding authors

^aInterBioscreen, Moscow, Russia

^bZelinsky Institute of Organic Chemistry, Leninsky Prospect, Moscow, Russia
E-mail: blich2006@mail.ru

^cSchool of Health, Department of Pharmacy, Aristotle University of Thessaloniki, Greece

^dMycological Laboratory, Department of Plant Physiology, Institute for Biological Research, Siniša Stanković, University of Belgrade, Bulevar Despota Stefana 142, Belgrade, Serbia

^eScientific Institute of Veterinary Medicine of Serbia, ul. Vojvode Toze 14, 11000 Belgrade, Serbia

Abstract

Usnic acid, a dibenzofuran, was originally isolated from lichens producing secondary metabolites, and is well known as an antibiotic, but is also endowed with several other interesting properties. Thus, the goal of this paper is the design of new usnic acid derivatives and evaluation of their antimicrobial activity. All newly synthesized compounds possess good antibacterial activity with MIC ranging from 1.02–50.93 × 10⁻² mmol mL⁻¹ and MBC from 2.05–70.57 × 10⁻² mmol mL⁻¹. The most sensitive bacterial species was Staphylococcus aureus, while Pseudomonas aeruginosa and Escherichia coli were the most resistant among the ATCC strains, and MRSA was the most resistant among all tested bacteria (ATCC and clinical isolates). Their antifungal activity was very strong (MIC = 0.35–7.53 × 10⁻² mmol mL⁻¹ and MFC = 0.70–15.05 × 10⁻² mmol mL⁻¹) – better than those of reference compounds and usnic acid itself. The most sensitive fungal species was Trichoderma viride, while Penicillium versicolor var. cyclopium appeared to be the most resistant. It should be mentioned that in general most of the compounds showed weaker antibacterial activity, but better antifungal properties than usnic acid itself. The results allow us to conclude that the title compounds are good lead compounds for novel more active antibacterial drugs. On the other hand, these compounds are very promising as antifungals.

https://pubs.rsc.org/en/content/articlelanding/2018/md/c8md00076j#!divAbstract

////////////Usnic acid, dibenzofuran

Structural evolution of carbon in an Fe@C catalyst during the Fischer–Tropsch synthesis reaction

ANTHONY CRASTO, organic chemistry, SYNTHESIS Comments Off

Feb 012019

Structural evolution of carbon in an Fe@C catalyst during the Fischer–Tropsch synthesis reaction

Shuai Lyu,^a^b Chengchao Liu,^b Guanghui Wang,*^a Yuhua Zhang,^b Jinlin Li^b and Li Wang*^b

Author affiliations

*Corresponding authors

^aHubei Key Laboratory of Coal Conversion and New Carbon Material, School of Chemical Engineering and Technology, Wuhan University of Science and Technology, Wuhan 430081, China
E-mail: wghwang@263.net

^bKey Laboratory of Catalysis and Materials Science of the State Ethnic Affairs Commission & Ministry of Education, South-Central University for Nationalities, Wuhan 430074, China
E-mail: li.wang@mail.scuec.edu.cn

Abstract

A pseudo-in situ research method was applied to provide insight into the structural evolution of carbon in an Fe@C catalyst at different stages of the Fischer–Tropsch reaction. Five typical stages of the catalyst were selected for in-depth structural investigation; these were: the fresh catalyst, reduced catalyst, and catalyst in the stable conversion period, in an increased-conversion period and at the inactivation stage. The results indicated that the integral structure of Fe@C constantly changed in the Fischer–Tropsch reaction. Iron carbide transformed from the Fe phase that was easily oxidized under high temperature Fischer–Tropsch conditions, and the carbon framework was completely destroyed in the reaction process, leading to a drastic decrease in the specific surface area of the material. This destruction could have two opposing effects: on the one hand, the loss of carbon could re-expose the active sites that have been covered by carbon at a reaction temperature of 320 °C and favor the reaction; on the other hand, the deposition of carbon could block the active sites and lead to inactivation when the reaction temperature is over 340 °C.

https://pubs.rsc.org/en/Content/ArticleLanding/2019/CY/C8CY02420K?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2Fcy+%28RSC+-+Catalysis+Science+%26+Technology+latest+articles%29#!divAbstract

////////Fischer–Tropsch

Telescoped Sequence of Exothermic and Endothermic Reactions in Multistep Flow Synthesis

FLOW CHEMISTRY, flow synthesis Comments Off

Jan 312019

A multistep sequential flow synthesis of isopropyl phenol is demonstrated, involving 4-step exothermic, endothermic, and temperature sensitive reactions such as nitration, reduction, diazotization, and high temperature hydrolysis. Nitration of cumene with fuming nitric acid produces 2- and 4-nitrocumene which are converted into respective cumidines by the hydrogenation using Pd/Ni catalyst in H-cube with gravity separation. Hydrolysis of in situ generated diazonium salts in the boiling acidic conditions is carried out using integration of flow and microwave-assisted synthesis. 58% of 4-isopropyl phenol was obtained. The sequential flow synthesis can be applied to synthesize other organic compounds involving this specific sequence of reactions.

Telescoped Sequence of Exothermic and Endothermic Reactions in Multistep Flow Synthesis

Yachita Sharma, Arun V. Nikam, and Amol A. Kulkarni*

Chemical Engineering & Process Development Division, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411008, India

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/acs.oprd.8b00008

Yachita Sharma

*Phone: +91-20-25902153, E-mail: aa.kulkarni@ncl.res.in.

Amol A. Kulkarni

Dr.Amol A. Kulkarni
Chemical Engineering & Process Development
CSIR-National Chemical Laboratory

Dr. Amol A. Kulkarni is a Scientist in the Chemical Engineering Division at the National Chemical Laboratory. He did his B. Chem. Eng. (1998), M. Chem. Eng (2000) and Ph.D. in chemical engineering (2003) all from the University Dept. of Chem. Technology (UDCT, Mumbai). In 2004 he worked at the Max Planck Institute-Magdeburg (Germany) as a Alexander von Humboldt Research Fellow. At NCL he is driving a research program on the design of microreactors and exploring their applications for continuous syntheses including of nanoparticles. He has been awarded with the Max-Planck-Visiting Fellowship from the Max-Planck-Society, Munich for 2008-2011. His research areas include: (i) design and applications of microreactors, (ii) design of multiphase reactors, (iii) experimental and computational fluid dynamics, and (iv) nonlinear dynamics of coupled systems. He is an active member of Initiative for Research and Innovation in Science (IRIS) supported by Intel’s Education Initiative to organize National Science Fair and popularize science in India.

Yachita Sharma

CSIR – National Chemical Laboratory, Pune

Location Pune, India

Department, Chemical Engineering and Process Development Division (NCL)

Yachita Sharma is a PhD student at CSIR-National Chemical Laboratory, Pune (India). She received her MSc in Applied Organic Chemistry in 2010. Her work focuses on exploring the continuous flow synthesis involving exothermic reactions and their integration.

Arun Nikam

CSIR – National Chemical Laboratory, Pune

Location, Pune, India

Department, Chemical Engineering and Process Development Division (NCL)

Email: arun11nikam@gmail.com

Arun was born and raised in Koregaon, Maharashtra, India. He completed his bachelors and masters in chemical sciences from Shivaji Unversity, Kolhapur, India. Currently, He is pursuing his Ph. D. under the supervision of Dr. Amol A. Kulkarni and Dr. B. L. V. Prasad. His work mainly focuses on flow synthesis of nanoparticles, drug formulation, and polymers. He develops new synthesis procedures and translates into flow chemistry to increase productivity with excellent control over the quality of the product. He is also exploring the application of nanoparticles in catalysis, electronics and pharmaceutical fields. He specializes in microwave-assisted continuous flow synthesis of nanomaterial and organic intermediate. Apart from his research, he actively pursues Yoga and spirituality. He also likes to play volleyball and has competed in inter CSIR tournaments.

/////////isopropyl phenol, flow chem,

“ALL FOR DRUGS” CATERS TO EDUCATION GLOBALLY, No commercial exploits are done or advertisements added by me. This is a compilation for educational purposes only. P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent

READ

ANTHONY MELVIN CRASTO

https://newdrugapprovals.org/

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE

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CALL +919323115463 INDIA

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Nickel-catalyzed regioselective C–H oxygenation: new routes for versatile C–O bond formation

spectroscopy, SYNTHESIS Comments Off

Jan 302019

Graphical abstract: Nickel-catalyzed regioselective CâH oxygenation: new routes for versatile CâO bond formation

Nickel-catalyzed regioselective C–H oxygenation: new routes for versatile C–O bond formation

Org. Chem. Front., 2019, Advance Article
DOI: 10.1039/C8QO01274A, Research Article

Ze-lin Li, Kang-kang Sun, Chun Cai
Nickel-catalyzed regioselective C–H oxygenation reactions of chelating arenes using iodobenzene diacetate, alcohols, and benzoic acids respectively as attacking reagents have been developed for the first time.
To cite this article before page numbers are assigned, use the DOI form of citation above.

Abstract

Nickel-catalyzed regioselective C–H oxygenation reactions of chelating arenes using iodobenzene diacetate, alcohols, and benzoic acids respectively as attacking reagents have been developed for the first time. Simplicity of operation, broad range of functional group tolerance, use of cheap transition metal nickel, and avoiding extraneous directing groups are the key features, thus providing an important complement to C–H oxygenation reactions and expanding the field of nickel-catalyzed C–H functionalizations. Explorations of mechanistic details are also described.

Nickel-catalyzed regioselective C–H oxygenation: new routes for versatile C–O bond formation

Ze-lin Li,^a Kang-kang Sun^a and Chun Cai*^a

Author affiliations

*Corresponding authors

^aCollege of Chemical Engineering, Nanjing University of Science & Technology, 200 Xiaolingwei, Nanjing, China
E-mail:c.cai@njust.edu.cn

https://pubs.rsc.org/en/Content/ArticleLanding/2019/QO/C8QO01274A#!divAbstract

2-(pyridin-2-yl)phenyl acetate (2a)

Formula: C13H11NO2 Mass: 213

To a mixture of 2-phenylpyridine (77.5 mg, 0.5 mmol) 1a, Ni(acac)2 (25.7 mg, 0.1 mmol, 20 mol %), ligand MePh2P (20.0 mg, 0.1 mmol, 20 mol %), and PhI(OAc)2 (483.2 mg, 0.75 mmol, 1.5 equiv) in a reaction tube was added solvent (CH3CN=2.0 mL). The reaction mixture was stirred at 115 °C for 24 h in air. Following the general procedure, 2a was purified by column chromatography on silica gel (petroleum ether: ethyl acetate = 5:1) as a white solid (80.9 mg, 76%).

1H NMR (500 MHz, Chloroform-d) δ 8.8 – 8.7 (m, 1H), 7.8 – 7.7 (m, 2H), 7.6 (dd, J = 7.9, 1.1 Hz, 1H), 7.5 (td, J = 7.7, 1.7 Hz, 1H), 7.4 (td, J = 7.5, 1.2 Hz, 1H), 7.3 – 7.3 (m, 1H), 7.2 (dd, J = 8.0, 1.2 Hz, 1H), 2.2 (s, 3H).

13C NMR (126 MHz, Chloroform-d) δ 168.4, 154.9, 148.6, 147.1, 135.3, 132.2, 129.8, 128.7, 125.4, 122.6, 122.3, 121.2, 20.0. GC-MS (EI) m/z: 213

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“ALL FOR DRUGS” CATERS TO EDUCATION GLOBALLY, No commercial exploits are done or advertisements added by me. This is a compilation for educational purposes only. P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent

READ

ANTHONY MELVIN CRASTO

https://newdrugapprovals.org/

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE

amcrasto@gmail.com

CALL +919323115463 INDIA

//////////////

A solvent-free catalytic protocol for the Achmatowicz rearrangement

green chemistry, spectroscopy, SYNTHESIS Comments Off

Jan 292019

Graphical abstract: A solvent-free catalytic protocol for the Achmatowicz rearrangement

Abstract

Reported here is the development of an environmentally friendly catalytic (KBr/oxone) and solvent-free protocol for the Achmatowicz rearrangement (AchR). Different from all previous methods is that the use of chromatographic alumina (Al₂O₃) allows AchR to proceed smoothly in the absence of any organic solvent and therefore considerably facilitates the subsequent workup and purification with minimal environmental impacts. Importantly, this protocol allows for scaling up (from milligram to gram), recycling of the Al₂O₃, and integrating with other reactions in a one-pot sequential manner.

A solvent-free catalytic protocol for the

Achmatowicz rearrangement

Guodong Zhao^a and Rongbiao Tong*^a^b

Author affiliations

*Corresponding authors

^aDepartment of Chemistry, The Hong Kong University of Science and Technology, Clearwater Bay, Kowloon, China
E-mail: rtong@ust.hk
Fax: +(852)23581594
Tel: +(852) 23587357

^bHKUST Shenzhen Research Institute, Shenzhen 518057, China

https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C8GC03030H?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

1n: colorless oil, 0.33 g, 73% yield for 2 steps.

1H-NMR (400 MHz, DMSO) δ: 7.59–7.58 (m, 1H), 7.45 (s, 2H), 6.40 (dd, J = 3.2, 1.8 Hz, 1H), 6.29 (d, J = 3.2 Hz, 1H), 5.49 (s, 1H), 4.74–4.60 (m, 1H), 4.18–4.07 (m, 2H), 2.09–2.04 (m, 2H).

13C-NMR (100 MHz, DMSO) δ: 157.6, 142.4, 110.7, 106.1, 66.5, 62.8, 35.2. IR (KBr) 3282.9, 2928.7, 1627.4, 1562.5, 1353.8, 1174.6, 1074.0, 999.7, 918.4, 742.8 cm-1 ;

HRMS (CI+ ) (m/z) calcd. for C7H11NO5S [M]+ 221.0352; found 221.0354.

2n (EtOAc/hexane = 3:1):colorless oil (dr 7:3), 46 mg, 97%.

1H-NMR (400 MHz, DMSO) δ: 7.48–7.47 (m, 2H), 7.34–7.02 (m, 2H), 6.12–6.03 (m, 1H), 5.61–5.48 (m, 1H), 4.60 (dd, J = 8.3, 4.1 Hz, 0.7H), 4.28 (ddd, J = 8.8, 4.0, 1.3 Hz, 0.3H), 4.20–4.11 (m, 2H), 2.27–2.20 (m, 1H), 1.97–1.86 (m, 1H).

13C-NMR (100 MHz, DMSO) δ: 196.7, 196.5, 151.9, 148.3, 127.7, 126.0, 90.9, 87.2, 74.6, 70.1, 65.8, 65.8, 30.3, 29.6. IR (KBr) 3370.4, 2987.0, 1689.5, 1364.3, 1268.0, 1178.4, 1023.3, 928.3, 755.1 cm-1 ;

HRMS (CI+ ) (m/z) calcd. for C7H11NO6S [M]+ 237.0302; found 237.0315.

////////////////Achmatowicz rearrangement

Eco-friendly decarboxylative cyclization in water: practical access to the anti-malarial 4-quinolones

spectroscopy, SYNTHESIS Comments Off

Jan 292019

Graphical abstract: Eco-friendly decarboxylative cyclization in water: practical access to the anti-malarial 4-quinolones

Abstract

An environmentally benign decarboxylative cyclization in water has been developed to synthesize 4-quinolones from readily available isatoic anhydrides and 1,3-dicarbonyl compounds. Isatins are also compatible for the reaction to generate 4-quinolones in the presence of TBHP in DMSO. This protocol provides excellent yields under mild conditions for a broad scope of 4-quinolones, and has good functional group tolerance. Only un-harmful carbon dioxide and water are released in this procedure. Moreover, the newly synthesized products have also been selected for anti-malarial examination against the chloroquine drug-sensitive Plasmodium falciparum 3D7 strain. 3u is found to display excellent anti-malarial activity with an IC₅₀ value of 33 nM.

Eco-friendly decarboxylative cyclization in water: practical access to the anti-malarial 4-quinolones

Yue Ma,^a Yongping Zhu,^a Dong Zhang,^a Yuqing Meng,^a Tian Tang,^a Kun Wang,^a Ji Ma,^a Jigang Wang^a and Peng Sun*^a

Author affiliations

*Corresponding authors

^aArtermisinin Research Center and Institute of Chinese Meteria Medica, Academy of Chinese Medical Sciences, Beijing, P. R. China
E-mail:psun@icmm.ac.cn

https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C8GC03570A?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

ethyl 2-(4-(benzyloxy)phenyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate (3u) White solid, m.p. 288-289 oC;

1H NMR (600 MHz, DMSO-d6) δ 12.14 (s, 1H), 8.13 (d, J = 8.0 Hz, 1H), 7.72 (ddd, J = 8.4, 7.1, 1.5 Hz, 1H), 7.64 (d, J = 8.3 Hz, 1H), 7.52 (td, J = 8.5, 1.7 Hz, 1H), 7.43 – 7.35 (m, 4H), 7.29 – 7.21 (m, 4H), 7.10 (td, J = 7.5, 0.5 Hz, 1H), 5.17 (s, 2H), 3.91 (q, J = 7.1 Hz, 2H), 2.00 (s, 1H), 0.83 (t, J = 7.1 Hz, 3H) ppm;

13C NMR (150 MHz, DMSO-d6) δ 174.1, 166.2, 156.2, 148.0, 139.8, 137.2, 132.8, 132.0, 130.5, 129.4, 128.7, 128.2, 127.6, 125.5, 125.2, 124.3, 123.6, 120.9, 118.9, 116.4, 115.8, 113.5, 70.2, 60.2, 14.0 ppm;

HRMS (ESI) calcd for [C25H21NO4+H]+ 400.1471, found 400.1463.

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Photo-organocatalytic synthesis of acetals from aldehydes

organic chemistry, spectroscopy, SYNTHESIS Comments Off

Jan 292019

Graphical abstract: Photo-organocatalytic synthesis of acetals from aldehydes

Abstract

A mild and green photo-organocatalytic protocol for the highly efficient acetalization of aldehydes has been developed. Utilizing thioxanthenone as the photocatalyst and inexpensive household lamps as the light source, a variety of aromatic and aliphatic aldehydes have been converted into acyclic and cyclic acetals in high yields. The reaction mechanism was extensively studied

Photo-organocatalytic synthesis of acetals from aldehydes

Nikolaos F. Nikitas,^a Ierasia Triandafillidi^a and Christoforos G. Kokotos*^a

Author affiliations

*Corresponding authors

^aLaboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece
E-mail:ckokotos@chem.uoa.gr

https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C8GC03605E?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

(3,3-Dimethoxypropyl)benzene (2a)6

Colorless oil; 95% yield; 1H NMR (200 MHz, CDCl3) δ: 7.33-7.18 (5H, m, ArH), 4.37 (1H, t, J = 5.8 Hz, OCH), 3.33 (6H, s, 2 x OCH3), 2.68 (2H, t, J = 7.6 Hz, CH2), 1.98- 1.87 (2H, m, CH2); 13C NMR (50 MHz, CDCl3) δ: 141.8, 128.4, 125.9, 103.7, 52.8, 34.0, 30.8; MS (ESI) m/z 181 [M+H]+ .

6. Q. Zhou, T. Jia. X.-X. Li, L. Zhou, C.-J. Li, Y. S. Feng, Synth. Commun., 2018, 48, 1068.

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Large scale synthesis of chiral (3Z,5Z)-2,7-dihydro-1H-azepine-derived Hamari ligand for general asymmetric synthesis of tailor-made amino acids.

spectroscopy, SYNTHESIS Comments Off

Jan 292019

(R)-2,2′-bis(bromomethyl)-1,1′-binaphthalene ((R)-17) was prepared in the identical manner and had identical analytical properties to those given here.

¹H NMR (400 MHz, CDCl₃): δ 4.25 (4H, s, 2 × CH₂), 7.07 (2H, dd, J = 8.4, 0.8 Hz, ArH), 7.27 (2H, ddd, J = 8.4, 6.8, 1.2 Hz, ArH), 7.48 (2H, ddd, J = 8.2, 6.8, 1.2 Hz, ArH), 7.74 (2H, d, J = 8.6 Hz, ArH), 7.92 (2H, d, J = 8.2 Hz, ArH), 8.02 (2H, d, J = 8.6 Hz, ArH).

¹³C NMR (100.6 MHz, CDCl₃): δ 32.6 (CH₂), 126.80 (ArCH), 126.82 (ArCH), 126.84 (ArCH), 127.7 (ArCH), 128.0 (ArCH), 129.4 (ArCH), 132.5 (quaternary ArC), 133.3 (quaternary ArC), 134.1 (quaternary ArC), 134.2 (quaternary ArC).

[α]²⁰_D = +173.8° (c = 1.0, CHCl₃).

An advanced process for large scale (500 g) preparation of a (3Z,5Z)-2,7-dihydro-1H-azepine-derived chiral tridentate ligand (Hamari ligand), widely used for asymmetric synthesis of tailor-made α-amino acids via the corresponding glycine Schiff base Ni(II) complex, is disclosed. The process includes amidation, bis-alkylation, and precipitation/purification of the target compound by TFA as a counterion.

Large Scale Synthesis of Chiral (3Z,5Z)-2,7-Dihydro-1H-azepine-Derived Hamari Ligand for General Asymmetric Synthesis of Tailor-Made Amino Acids

Motohiro Takahashi*^†

, Hiroki Moriwaki^†, Toshio Miwa^†, Brittanie Hoang^‡, Peng Wang^‡, and Vadim A. Soloshonok*^§^∥

^† Hamari Chemicals Ltd., 1-4-29 Kunijima, Higashi-Yodogawa-ku, Osaka 533-0024, Japan

^‡ Hamari Chemicals USA, San Diego Research Center, 11494 Sorrento Valley Road, San Diego, California 92121, United States

^§ Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, 20018 San Sebastián, Spain

^∥ IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, Plaza Bizkaia, 48013 Bilbao, Spain

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/acs.oprd.8b00406

Publication Date (Web): January 18, 2019

*E-mail: motohiro-takahashi@hamari.co.jp., *E-mail: vadym.soloshonok@ehu.es.

This article is part of the Japanese Society for Process Chemistry special issue.

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