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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc 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 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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India’s Strides to buy Aspen’s Australian generic pharmaceutical business


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India’s Strides to buy Aspen’s Australian generic pharmaceutical business
India-based Strides Arcolab has signed an agreement with subsidiaries of South African drugmaker Aspen Pharmacare Holdings to acquire its generic pharmaceutical business in Australia and certain branded pharmaceutical assets for around A$380m ($300m).

see

http://www.pharmaceutical-technology.com/news/newsindias-strides-buy-aspens-australian-generic-pharmaceutical-business-4583399?WT.mc_id=DN_News

  About Strides

  • picHeadquartered in India, Strides Arcolab is a pharmaceutical company with a key focus on development and manufacture of IP-led niche generics and bio-pharmaceuticals. It is also among the world’s largest manufacturers of specialty soft gelatin capsules. With world-class manufacturing facilities, an innovative R&D hub in Bangalore and a strong commercial platform to market branded and commodity generics globally, Strides has earned a reputation for building and scaling profitable businesses in a short span of time.

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Chandos Street, St Leonards

 

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Lupin buys Brazilian pharmaceutical firm Medquímica


 

Lupin buys Brazilian pharmaceutical firm Medquímica
India-based drugmaker Lupin has acquired 100% equity interest in Brazilian pharmaceutical firm Medquímica Indústria Farmacêutica.

read at

http://www.pharmaceutical-technology.com/news/newslupin-buys-brazilian-pharmaceutical-firm-medqumica-4578219?WT.mc_id=DN_News

Group president and CEO, Lupin Pharmaceuticals, and director on the board of Lupin Limited, Vinita Gupta

Medquímica

.

A Medquímica Indústria Farmacêutica é uma empresa genuinamente brasileira que atua na produção de medicamentos para o uso humano. Com sua linha de produção instalada em Juiz de Fora, a Medquimica está presente em todo o Brasil através de seus representantes.

Working in syntony with the market. There are 30 years that it is the north that takes the Medquímica Pharmaceutical Industry Ltda. to dedicate to the production of pharmaceutical products of proven effectiveness and certain return for all its net of customers. For such, the Medquímica invests in physical and human resources, forming a qualified and highly experienced technical team, who detaches in the marketplace for producing medicines of uncontestable quality and trustworthiness.

With the quality certified through the Good Practical of Manufacture, the Medquímica detaches for having a laboratory of reference inside its installations. Moreover, respecting the resolution 134 from Anvisa, gradually, all its medicines are being evaluated for the tests of pharmaceutical equivalence, proving, in this way, the quality of Medquímica’s product. Such actions had resulted in a supported growth of credibility and sales.

For giving support to all this development, the Medquímica will start the construction of the first projected national plant in the most rigorous and recent requirements of the ANVISA. Thirty years of history, qualified technician team, tests of equivalence and bioequivalência and a model plant makes from Medquímica the certain alternative for the success of its businesses

Fábrica:
(32) 3224-4087 (Telefax)

Administração:
(32) 2101-4000 (Telefax)

The Medquímica Pharmaceutical Industry is a genuinely Brazilian company that acts in the medicine production for the human use. With its line of production installed in Juiz de Fora, the Medquimica is present in all over Brazil through its representatives.

Industry
Rua Otacílio Esteves da Silva, 40
Bairro Granjas Betânia
CEP: 36047-400
Juiz de Fora – MG

Administration
Rua Fernando Lamarca, 255
Bairro Distrito Industrial
CEP: 36092-030
Juiz de Fora – MG

Juiz de Fora

Map of juiz de fora

Paço Municipal de Juiz de Fora

 

No todo parece bem interessante. Dá pra tirar muitas fotos boas. Já teve outro thread bem legal sobre a cidade.

 

 

 

 

 

Daiichi partners with AZ to sell Movantik in US…….Pharmatimes, Selina McKee


Naloxegol.svg
Naloxegol
Daiichi partners with AZ to sell Movantik in US 
March 19, 2015

Selina McKee

News editor, Selina McKee

Selina McKee

Qualified from King’s College London with BSc (hons) in Human Biology in 1999 with an interest in medical journalism. Has since held positions as a database analyst managing a portfolio of companies at Evaluate Pharma, and as news editor at Pharma Marketletter. Fluent German speaker, interests include music, piano, reading, astronomy, photography and Formula 1.

Daiichi partners with AZ to sell Movantik in US

AstraZeneca has chosen Daiichi Sankyo to help sell its novel constipation drug Movantik (naloxegol) in the US, as the firm gears up for its launch in April.

First-in-class Movantik was cleared in the US last September for the treatment of opioid-induced constipation in adults with chronic non-cancer pain, for which there is still significant unmet need.

PharmaTimes Magazine and Digital offer a unique blend of news stories, interviews, features, case studies, analysis and comment on the critical issues facing the pharma and healthcare sectors. Our wide editorial lens combined with our editorial philosophy to deliver sharp, informed and entertaining coverage from the perspective of the industry, the payer and the patient, allows PharmaTimes to help kickstart conversations that matter most to our audience of decision makers within pharma and the healthcare profession.PharmaTimes Competitions are a critical facet of our business, providing a unique opportunity for industry to showcase its most talented people in marketing, communications, sales and clinical research. No other competitions offer entrants the chance to compete head-to-head in real-life challenges devised by independent industry and healthcare experts, to test their skill sets against their peers in real time, and receive feedback to ensure the whole experience is a valuable learning process.

 Selina McKee

Selina McKee

Editor, UK News at PharmaTimes

London, United Kingdom
Pharmaceuticals
uk.linkedin.com/pub/selina-mckee/4/174/339/en

Experience

Editor, UK News

PharmaTimes

September 2005 – Present (9 years plus

Company News Editor

Pharma Marketletter

November 2003 – August 2005 (1 year 10 months)

Research Analyst

Evaluate Pharma

March 2000 – January 2003 (2 years 11 months)

Education

King’s College London, U. of London

BSc (Hons) Human Biology

1996 – 1999

PharmaTimes Media Ltd.
8-10 Dryden Street
Covent Garden
London WC2E 9NA

Email: pharma@pharmatimes.com
Telephone: +44 (0)20 7240 6999
Fax: +44 (0)20 7240 4479

Company Registration Number: 09019637

Selina McKee

Map of Dryden St, London WC2E 9NA, UK
Dryden St London WC2E 9NA, UK

Registered in England & Wales at:
PharmaTimes Media Limited
8-10 Dryden Street
Covent Garden
London WC2E 9NA

more………….

LINKEDIN

uk.linkedin.com/pub/selina-mckee/4/174/339/en

Authors – PharmaTimes

Selina McKee. Qualified from King’s College London with BSc (hons) in Human Biology in 1999 with an interest in medical journalism. Has since held positions .

Selina McKee (@PTSelinaMcKee) | Twitter

The latest Tweets from Selina McKee (@PTSelinaMcKee). News Editor for http://t.co/o6l54nzsxb & PharmaTimes Magazine. Also on your mobile. Sussex, UK.

5 Dryden Street, Covent Garden, London. London – , Greater London, WC2

Covent Garden Interior May 2006

covent garden. 2 Dryden Street. London

Dryden Street, London
.
Happy Hands provides domestic cleaning in Covent Garden (WC2) and other districts in London.

Suven Life gets patent for neuro-degenerative drug


March 16, 2015

Drug firm Suven Life Sciences has been granted a patent each by the US and New Zealand for a drug used in the treatment of neuro-degenerative diseases.

The patents are valid until 2030 and 2031, respectively, Suven Life Sciences said in a filing to the BSE.

Commenting on the development, Suven Life CEO Venkat Jasti said: “We are very pleased by the grant of these patents to Suven for our pipeline of molecules in CNS arena that are being developed for cognitive disorders with high unmet medical need with huge market potential globally.”

SUVEN, Chief executive and chairman Venkat Jasti

The company has “secured patents in USA and New Zealand to one of their new chemical entity (NCE) for CNS therapy through new mechanism of action – H3 Inverse agonist…,” Suven Life Sciences said.

With these new patents, Suven has a total of 20 granted patents from US and 23 granted patents from New Zealand.

“These granted patents are exclusive intellectual property of Suven and are achieved through the internal discovery research efforts.

“Products out of these inventions may be out-licensed at various phases of clinical development like at Phase-I or Phase-II,” Suven said.

Pdf Link: Suven Life Sciences secures 2 (two) Product Patents for their NCE’s through New mechanism of action – H3 Inverse Agonist in USA & New Zealand

http://www.bseindia.com/xml-data/corpfiling/AttachLive/suven_life_sciences_ltd_160315.pdf

Suven Life Sciences secures 2 (two) Product Patents for their NCE’s through New mechanism of action – H3 Inverse Agonist in USA & New Zealand HYDERABAD, INDIA (March 16, 2015) – Suven Life Sciences Ltd (Suven) announced today that they secured patents in USA (us 8912179) and New Zealand (614567) to one of their New Chemical Entity (NCE) for CNS therapy through new mechanism of action – H3 Inverse agonist and these patents are valid until 2030 and 2031 respectively. The granted claims of the patent include the class of selective H3 ligands discovered by Suven and are being developed as therapeutic agents and are useful in the treatment of cognitive impairment associated with neurodegenerative disorders

 

Suven Life Sciences Ltd.
6th Floor, SDE Serene Chambers,
Avenue – 7, Road No. 5, Banjara Hills,
Hyderabad-500 034, Telangana, INDIA

Phone : +91-40-2354-1142, 2354-3311
Fax     : +91~40~2354-1152
Email id: info@suven.com

 

INDIAN PATENT

 

  • Nirogi, Ramakrishna; Shinde, Anil Karbhari; Kambhampati, Ramasastri; Namala, Rambabu; Dwarampudi, Adi Reddy; Kota, Laxman; Gampa, Murlimohan; Kodru, Padmavathi; Tiriveedhi, Taraka Naga Vinaykumar; Kandikere, Vishwottam Nagaraj; et al
  • From Indian Pat. Appl. (2012), IN 2010CH02551

 

 

 

PATENT

http://www.google.com/patents/US8912179

The present invention relates to heterocyclyl compounds of formula (I) and their pharmaceutically acceptable salts, its process of preparation and compositions containing them, for the treatment of various disorders that are related to Histamine H3 receptors.

Figure imgf000003_0001
ONE EXAMPLE
EXAMPLE 1
Example 1
Preparation of 1-[2-(1-Cyclobutyl-piperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]-propan-1-one tartrate
Step (i): Preparation of 2-(1-Cyclobutyl-piperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridine-5-carboxylic acid tert-butyl ester

1-Cyclobutyl-piperidin-4-ol (1.6 grams, 10 mmol) in tetrahydrofuran (20 mL) was treated with cooled and stirred suspension of sodium hydride (0.9 grams, 18 mmol) in tetrahydrofuran (20 mL) slowly over a period of 30 minutes; the reaction mixture was stirred for 1 hour. A solution of 2-Bromo-6,7-dihydro-4H-thiazolo[5,4-c]pyridine-5-carboxylic acid tert-butyl ester (3 grams, 9 mmol, obtained in preparation 1) in tetrahydrofuran (30 mL) was added drop wise over a period of 15 minutes and refluxed the reaction for 6 hours. Reaction mass was quenched with ice cold water and the product was extracted with ethyl acetate (3×50 mL). Combined organics were washed with water followed by brine and dried over anhydrous sodium sulphate. Organic volatiles were evaporated under vacuum. The residue was purified by flash chromatography (ethylacetate/n-hexane, 1/1) to obtain the title compound (2.0 grams).

1H-NMR (δ ppm): 1.48 (9H, s), 1.65-1.72 (2H, m), 1.85-1.92 (4H, m), 2.01-2.07 (4H, m), 2.18-2.19 (2H, m), 2.57 (2H, m), 2.62-2.66 (2H, m), 2.71-2.75 (1H, m), 3.70 (2H, m), 4.43 (2H, m), 4.93 (1H, m);

Mass (m/z): 394.2 (M+H)+.

Step (ii): Preparation of 2-(1-Cyclobutyl-piperidin-4-yloxy)-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridineA solution of 2-(1-Cyclobutyl-piperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridine-5-carboxylic acid tert-butyl ester (2.0 grams, 5 mmol, obtained in above step) in dichloromethane (30 mL) was treated with trifluroacetic acid (5.0 mL, 50 mmol) at 0° C. Reaction mass was stirred for 4 hours. After completion of reaction, the reaction mass was quenched into ice cold water and adjust pH to 10, by using 40% aqueous sodium hydroxide solution. The product was extracted with dichloromethane (3×50 mL), combined organics were washed with water followed by brine and dried over anhydrous sodium sulphate. Organic volatiles were evaporated under vacuum to obtain the title compound (1.3 grams).

1H-NMR (δ ppm): 1.68-1.74 (2H, m), 1.85-1.93 (4H, m), 2.06 (4H, m), 2.19 (2H, m), 2.60-2.61 (4H, m), 2.73-2.80 (1H, m), 2.90-3.10 (1H, m), 3.13-3.16 (2H, m), 3.85 (2H, s), 4.90-4.93 (1H, m);

Mass (m/z): 294.2 (M+H)+.

Step (iii): Preparation of 1-[2-(1-Cyclobutyl-piperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]-propan-1-oneA solution of 2-(1-Cyclobutyl-piperidin-4-yloxy)-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine (1.3 grams, 4 mmol, obtained in above step) and triethylamine (1.9 mL, 13 mmol) in dichloromethane (30 mL) was cooled to 0° C. Propionylchloride (0.4 mL, 5 mmol) in dichloromethane (5 mL) was added drop wise over a period of 15 minutes and stirred the reaction for 30 minutes. Reaction mass was poured onto ice cold water and the product was extracted with ethyl acetate (3×50 mL). Combined organics were washed with water followed by brine and dried over anhydrous sodium sulphate. Organic volatiles were evaporated under vacuum. The residue was purified by flash chromatography (methanol/chloroform, 2/98) to obtain the title compound (1.0 gram).

1H-NMR (δ ppm): 1.17-1.21 (3H, m), 1.65-1.72 (5H, m), 1.87-1.91 (4H, m), 2.01-2.07 (4H, m), 2.22 (1H, m), 2.38-2.45 (2H, m), 2.45 (1H, m), 2.68-2.76 (3H, m), 3.72-3.74 (1H, m), 4.47-4.62 (2H, m), 4.92-4.94 (1H, m).

Mass (m/z): 350.4 (M+H)+.

Step (iv): Preparation of 1-[2-(1-Cyclobutyl-piperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]-propan-1-one tartrateA solution of 1-[2-(1-Cyclobutyl-piperidin-4-yloxy)-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]-propan-1-one (0.8 grams, 2.3 mmol, obtained in above step) in methanol (10 mL) was treated with L(+)-Tartaric acid (0.34 grams, 2.3 mmol) at 0° C. Stirred the reaction mass for about 1 hour and the solvent was evaporated under vacuum to dryness. The solids were washed with diethyl ether and dried under vacuum to obtain the title compound (1.1 grams).

1H-NMR (δ ppm): 1.12-1.20 (3H, m), 1.82-1.87 (2H, m), 2.16-2.32 (7H, m), 2.45-2.55 (2H, m), 2.63-2.66 (3H, m), 2.72 (1H, m), 3.20 (2H, m), 3.47-3.50 (1H, m), 3.66-3.70 (1H, m), 3.81-3.88 (2H, m), 4.45 (2H, s), 4.60 (2H, s), 5.18 (5H, m);

Mass (m/z): 350.4 (M+H)+.

Publication number US8912179 B2
Publication type Grant
Application number US 13/818,152
PCT number PCT/IN2010/000740
Publication date Dec 16, 2014
Filing date Nov 15, 2010
Priority date Sep 2, 2010
Also published as CA2812970A1, 4 More »
Inventors Ramakrishna Nirogi, Anil Karbhari Shinde,Ramasastri Kambhampati, Rambabu Namala,Adi Reddy Dwarampudi, Laxman Kota,Murlimohan Gampa, Padmavathi Kodru,Taraka Naga Vinaykumar Tiriveedhi,Vishwottam Nagaraj Kandikere, Nageshwara Rao Muddana, Ramanatha Shrikantha Saralaya, Pradeep Jayarajan, Dhanalakshmi Shanmuganathan, Ishtiyaque Ahmad,Venkateswarlu Jasti, Less «
Original Assignee Suven Life Sciences Limited
Export Citation BiBTeX, EndNote, RefMan
External Links: USPTO, USPTO Assignment, Espacenet

……………….

Banjara Hills,Hyderabad

Banjara Hills, Hyderabad, Telangana
Map of Banjara Hills, Hyderabad
TAJ KRISHNA
SUBWAY RESTAURANT

Sun Pharma to acquire GSK’s Australian opiates business


Sun Pharma to acquire GSK’s Australian opiates business

India-based Sun Pharmaceutical Industries has agreed to acquire GlaxoSmithKline’s (GSK) opiates business in Australia.

The agreement has been signed by wholly-owned subsidiaries of both firms, with the financial terms not disclosed.

Sun Pharma API business executive vice-president Iftach Seri said: “The global opiates market holds good potential and the addition of GSK’s Opiates business will strengthen our positioning further.”

http://www.pharmaceutical-technology.com/news/newssun-pharma-to-acquire-gsks-australian-opiates-business-4524031?WT.mc_id=DN_News

http://indianexpress.com/article/business/business-others/sun-pharma-to-buy-gsks-opiates-biz-in-australia/

Sun Pharmaceutical Industries Ltd(SUN.NS), India’s largest drugmaker by sales, said on Tuesday it has agreed to buy GlaxoSmithKline’s(GSK.L) opiates business in Australia to strengthen its pain management portfolio.

The business consists of analgesics made from raw materials found in opium poppy plants, and includes two manufacturing sites in the states of Tasmania and Victoria.

Financial details of the deal were not disclosed. A Sun Pharma spokesman declined to comment. Glaxo did not immediately respond to a request seeking comment.

Glaxo supplies a quarter of the world’s medicinal opiate needs from poppies grown by farmers in Tasmania, according to the company website. The company’s Australian opiates business brought in revenue of A$89 million ($69.63 million) in 2013.

Australia’s poppy industry is the world’s largest legal supplier of pharmaceutical grade opiates for painkillers, and Glaxo is one of three firms that control the crop and production in Tasmania.

The other two are Johnson & Johnson’s (JNJ.N) unit Tasmanian Alkaloids, and privately-held TPI Enterprises.

Glaxo’s decision to part with the opiates business comes as Tasmania’s poppy industry is facing a tough crop and the United Nations is expected to cut the state’s poppy crop area this week.

Glaxo said the deal would allow it to “focus on delivering its innovative product portfolio” in Australia.

“The opiates business has been an important part of our Australian business for many years, but as our portfolio transitions, we believe now is the right time to hand this business over to someone else,” Steve Morris, general manager of GSK Opiates, said in a statement.

The business employs 185 staff, including 155 in Victoria state and 30 in Tasmania state. Sun Pharma said it would hire all employees from both sites.

“The acquisition is a part of our strategy towards building our portfolio of opiates and accessing strong capabilities in this segment,” said Iftach Seri, executive vice president of the active pharmaceuticals ingredients business at Sun Pharma.

Both companies said they expect to close the deal by August.

Sun Pharma shares closed 1.93 percent higher on Tuesday, while the broader Nifty rose 0.44 percent.

($1 = 1.2781 Australian dollars)

Lupin and Celon Pharma partner for generic version of GSK’s Advair Diskus


 

Vinita Gupta, 43, Group President and CEO, Lupin Pharmaceuticals and Director, Lupin

India-based drugmaker Lupin has signed an agreement with Polish biopharmaceutical firm Celon Pharma to develop a fluticasone / salmeterol dry powder inhaler (DPI).

Under the deal, Lupin will take the responsibility for commercialisation of the product, which is a generic version of GlaxoSmithKline’s (GSK) Advair Diskus.

Lupin CEO Vinita Gupta said: “We are very pleased to partner with Celon given their experience in the development and manufacturing of fluticasone/salmeterol DPI in Europe…………..http://www.pharmaceutical-technology.com/news/newslupin-celon-pharma-partner-generic-version-gsks-advair-diskus-4514718?WT.mc_id=DN_News

Vinita Gupta, 43, Group President and CEO, Lupin Pharmaceuticals and Director, Lupin, is based in the United States, but has been in India a lot in the past one year.

Vinita Gupta, 43, Group President and CEO, Lupin Pharmaceuticals and Director, Lupin,
Vinita Gupta

With an expanding role in Lupin’s universe, Vinita has been spending more time outside the US, at times taking her six-year-old son, Krish with her. “He is getting exposure at a much younger age,” she says. Gupta herself was exposed to business at the age of 11 by her father Desh Bandhu Gupta, Lupin’s founder and Chairman.

“We almost had a family board at home, discussing work,” she says. Currently work goes well indeed, with Gupta taking new initiatives in India and also making the business more global. “I am focusing on drivers for growth in our business for the next five years,” she says.

Gupta is married to US-based businessman Brij Sharma.

 

 

 

 

DB Gupta (centre) Chairman, Vinita Gupta (right) CEO and Nilesh Gupta

 

Route Design in the 21st Century: The ICSYNTH Software Tool as an Idea Generator for Synthesis Prediction


Figure

 

The new computer-aided synthesis design tool ICSYNTH has been evaluated by comparing its performance in predicting new ideas for route design to that of historical brainstorm results on a series of commercial pharmaceutical targets, as well as literature data. Examples of its output as an idea generator are described, and the conclusion is that it adds appreciable value to the performance of the professional drug research and development chemist team.

Chemical Development, AstraZeneca R&D, Silk Road Business Park, Macclesfield, SK10 2NA Cheshire, U.K.
Chemnotia AB, Forskargatan 20 J, 151 36 Södertälje,Sweden
§ InfoChem GmbH, Landsberger Straße 408/V, D-81241 München, Germany
Org. Process Res. Dev., Article ASAP
DOI: 10.1021/op500373e
Publication Date (Web): January 22, 2015
Copyright © 2015 American Chemical Society
*(H.-J.F.) E-mail: Hans-Jurgen.Federsel@astrazeneca.com., *(M.G.H.) E-mail: mghutchings@infochem.de.
Currently, ICSYNTH has assumed a place as a unique predictive tool for route design in Chemical Development in AZ. While it is finding valuable commercial application in our own and others’ hands, it remains a work in progress.
ICsynthInfoChem’s powerful synthesis planning tool now in Version 2.0. Read more …

InfoChem will be represented at the forthcoming ACS Meeting in San Diego. You will find Dr. Josef Eiblmaier, Dr. Valentina Eigner Pitto, and Dr. Peter Loew …
ICSYNTH
InfoChem’s ICSYNTH is a powerful computer aided synthesis design tool that enables chemists to generate synthetic pathways for a target molecule. The benefit is that ICSYNTH can facilitate innovation by stimulating ideas for alternative or novel synthetic routes that otherwise may not be considered. This may lead to improved route design, for example shorter pathways or more economical reaction modifications.

After inputting the target, users can select different synthetic strategies depending on requirements. ICSYNTH then automatically generates a multistep interactive synthesis tree – each node on the tree representing a precursor. The advantages are that the suggested reactions are based on, and linked to, published reactions (or their analogs) and the precursor availability is automatically checked in commercial catalogs. Users can modify the synthesis tree or select precursors for further analysis.

At the heart of ICSYNTH is an algorithmic chemical knowledge base of transform libraries that are automatically generated from reaction databases. The number of transform libraries is only limited by the availability of validated reaction databases.
In addition to retro synthesis design, ICSYNTH has a forward reaction prediction module that offers reactivity mapping for the target molecule. Version 2.0 of ICSYNTH was launched in April 2014. The completely re-designed user interface (based on JavaScript) and major improvements in the algorithm responsible of the precursor search are the main enhancements of Version 2.0. In addition the forward reaction prediction algorithm has been optimized. Click here to see a complete version history.

INFOCHEM GESELLSCHAFT FÜR CHEMISCHE INFORMATION MBH

Landsberger Straße 408/V
D-81241 München
Germany

Phone: +49 (0)89 58 30 02
Fax: +49 (0)89 580 38 39
Email: info@infochem.de

 

Historische Bilder der Landsberger Straße – An der Trambahnhaltestelle Holzapfelstraße endet – Münchner Straßen – München – Süddeutsche.de

 

A Novel and Practical Synthesis of Ramelteon


Ramelteon.svgRAMELTEON
Abstract Image

An efficient and practical process for the synthesis of ramelteon 1, a sedative-hypnotic, is described. Highlights in this synthesis are the usage of acetonitrile as nucleophilic reagent to add to 4,5-dibromo-1,2,6,7-tetrahydro-8H-indeno[5,4-b]furan-8-one 2 and the subsequent hydrogenation which successfully implement four processes (debromination, dehydration, olefin reduction, and cyano reduction) into one step to produce the ethylamine compound 13where dibenzoyl-l-tartaric acid is selected both as an acid to form the salt in the end of hydrogenation and as the resolution agent. Then, target compound 1 is easily obtained from13 via propionylation. The overall yield in this novel and concise process is almost twice as much as those in the known routes, calculated on compound 2.

A Novel and Practical Synthesis of Ramelteon

State Key Lab of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, State Institute of Pharmaceutical Industry, Shanghai 200437,China
Org. Process Res. Dev., Article ASAP
DOI: 10.1021/op500386g

http://pubs.acs.org/doi/abs/10.1021/op500386g

Publication Date (Web): January 6, 2015
Copyright © 2015 American Chemical Society
*Telephone: +86 21 55514600. E-mail: zhouweicheng58@163.com.
Preparation of (S)-N-[2-(1,6,7,8-Tetrahydro-2H-indeno[5,4-b] furan-8-yl)ethyl]propionamide(1).
GAVE
white solid of 1(1.570 g, 85% yield, 99.8% ee). Purity by HPLC 99.6%.
Mp: 115−116 °C(113−115°C in literature 1 ).
Ramelteon.svg
1 H−NMR(400 MHz, CDCl3):
δ 1.39 (t, 3H); 1.63 (m, 1H); 1.83 (m, 1H); 2.02 (m, 1H); 2.16 (dd, J=8, 2H); 2.28 (m, 1H); 2.78 (m, 1H); 2.83 (m, 1H); 3.14 (m, 1H); 3.22 (m, 2H); 3.33 (m, 2H); 4.54 (m, 2H); 5.38 (br s, 1H); 6.61 (d, J=8, 1H); 6.97 (d, J=8, 1H).
Ramelteon.svg
13C−NMR(100 MHz, CDCl3):
δ 173.85, 159.56, 143.26, 135.92, 123.52, 122.28, 107.56, 71.26, 42.37, 38.17, 33.66, 31.88, 30.82, 29.86, 28.73, 10.01.
MS (ES+): m/z 282(M+Na) + .
[α]D −57.3(c=1.0, CHCl3, −57.8 in literature 1 ).
Anal. (C16H21NO2) Calc: C, 74.10; H, 8.16; N, 5.40; found: 74.09; H, 8.17; N, 5.47.
References
(1) Uchikawa, O.; Fukatsu, K.; Tokunoh, R.; Kawada, M.; Matsumoto, K.; Imai, Y.; Hinuma, S.; Kato, K.; Nishikawa, H.; Hirai, K.; Miyamoto M.; Ohkawa, S. J. Med. Chem. 2002, 45, 4222-4239.
(2) Yamano, T.; Yamashita, M.; Adachi, M.; Tanaka, M.; Matsumoto, K.; Kawada, M.; Uchikawa, O.; Fukatsu, K.; Ohkawa, S. Tetrahedron: Asymmetry. 2006, 17, 184-190.
SHANGHAI
SHANGHAI CHINA
The Shanghai International Exhibition Center, an example of Soviet neoclassical architecture in Shanghai

Pi-Process Intensification Experts LLP at CPhI Mumbai India 3rd Dec 2014…My visit


 

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I (Dr Anthony) seated with Dr Vijay Kirpalani CEO of Pi-Process Intensification Experts LLP
at CPhI Mumbai India 3rd Dec 2014
Pi-Process Intensification Experts LLP
provide

Process Intensification

Creating competitive advantage through Improved and consistent quality, high efficiencies and maximum flexibility.

Safer, Cleaner, Smaller, Cheaper and Smarter processes , The basic principle of Process Intensification is to fit the equipment to the process and not process to the equipment, as is the case now.

Process Intensification can achieve drastic improvement in the time cycle and yields as well as converting batch processes to continuous process using specialized set of equipment. The design philosophy in process intensification is to design a process which has Chemical Kinetics as its only limitation. See the illustration below

“Process Intensification by Kinetics alone controlling the reaction, using specialized equipments; modification / telescoping of process steps achieves drastic reduction in time cycles and converts batch processes to continuous ; Reduced energy consumption, Reduced by-product formation; sustainability , hazard-containment, compliance to QbD and PAT and importantly a much faster time-to-market”

Illustrative examples are as follows:

  • Watt’s aldol reaction: Time needed to reach 100 % conversion 20 minutes against 24 hours in batch process
  • Fisher Esterification: Pi gives 83% yield against 15% in batch process
  • Grignard Reaction: Pi gives 78% yield against 49% in batch process
  • Nitration Reaction: Product purity increase from 56% to 78% and yield of mononitrate increases 55% to 75%.
Benefits of Process Intensification (PI) Techniques

Benefits of Process Intensification (PI) Techniques

Sponsored Projects

Scale-up for Retrofitting in existing plant as well as greenfield projects based on flow chemistry data generated in our laboratory. A well-equipped Laboratory and Pilot Plant set-up is available at our “Pi-Lab” for carrying out “FLOW Chemistry” based Reactions and utilizing numerous Process Intensification techniquesfor Unit-Processes & Unit-Operations for the industry to reap the benefits of Process Intensification.

The laboratory and pilot plant data will be utilized to provide the plant scale design using specialized equipments like micro-reactors, micro-plate-reactors in SiC, monolithic loop reactors, spinning disk reactors-cum-heat exchangers, FUMI reactors, dynamic mixing reactors, oscillatory baffled reactors (OBR), Bio-catalytic impregnated membrane Reactors, and other modern state-of-the-art equipments enabling conversion of batch to continuous flow processes.

We handle hazardous chemistries with very high exotherms (upto 1300 J/gm) safely in the range of -70oC to + 250oC with pressures upto 200 bar, and with reaction times from 0.03 sec to 1 hour and reactor volumes from 0.2 ml to 100 ml (Lab) and 1 L (Pilot) — yielding from 20 gms to 8 Kgs/hour (Lab) and 500 gms to 200 Kgs/hour (Pilot).


Scale Up – Flexibility & Adaptability

Pi …… will provide all the services for scale up to the sizes desired by clients by utilizing data from Laboratory trials.

Rental

A range of Flow Chemistry and Process Intensification equipments can be offered on rent. This enables the users to get the hands-on experience so as to select the apt equipments for their needs.

Vijay Kirpalani
CEO
Pi-Process Intensification Experts LLP
Plot-W-33,  M.I.D.C. Industrial Area
TALOJA – 410208, Navi Mumbai, INDIA
email : vk@pi-inc.co
www.pi-inc.co
Tel: +91-9321342022 // +91-9821342022

some pics from hall 5 -H-47 at cphi mumbai india dec 3 2014

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CphI-2014-Fa

 

 

Glenmark bags two accolades at Pharmexcil Awards 2014


Glenmark bags two accolades at Pharmexcil Awards 2014

read

http://www.biospectrumasia.com/biospectrum/news/219103/pharmexcil-announces-outstanding-exports-awards

 

read at

http://www.glenmarkpharma.co.za/blog/glenmarks-bags-2-gold-accolades-at-pharmexcil-awards-2014