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At Scientific Update Organic Process Research and Development Conference, NCL, PUNE, INDIA, 5 TH DEC 2014
I am seated left with DR PAUL MURRAY, DR JOHN KNIGHT, DR WILL WATSON, At Scientific Update Organic Process Research and Dev Conference, NCL, PUNE ,INDIA, 5 TH DEC 2014
DR WILL AND DR JOHN IN A DISCUSSION
A SLIDE
PROCESS CHEMISTRY CONFERENCES SCHEDULE
EVENT
- Title:
- Organic Process Research & Development – India
- Subtitle:
- The 32nd International Conference and Exhibition
- When:
- 04.12.2014 – 05.12.2014
- Where:
- National Chemical Laboratory – Pune
- Brochure:
- View Brochure
poster by DR PRAVIN KENDREKAR
PUNE CITY
NCL
MUMBAI PUNE EXPRESSWAY
PUNE FC
Volkswagen India Plant and offices in Pune
From top: Fergusson College, Mahatma Gandhi Road(left), Shaniwarwada (right), the HSBC Global Technology India Headquarters, and the National War Memorial Southern Command
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Welcome Scientific update to Pune, India 2-3 and 4-5 Dec 2014 for celebrating Process chemistry
WEBSITE http://www.scientificupdate.co.uk/
SCIENTIFIC UPDATE HAS A REPUTATION FOR ITS HIGH QUALITY EVENTS, BOTH FOR THE SCIENTIFIC CONTENT AND ALSO FOR THE EFFICIENCY OF ITS ORGANISATION. KEEP YOUR SKILLS UP TO DATE AND INVEST IN YOUR CONTINUING PERSONAL PROFESSIONAL DEVELOPMENT.
TRAINING COURSE 2-3 DEC 2014
Process Development for Low Cost Manufacturing
When:02.12.2014 – 03.12.2014
Tutors:
Where: National Chemical Laboratory – Pune, India
Brochure:View Brochure
Register http://scientificupdate.co.uk/training/scheduled-training-courses.html
DESCRIPTION
Chemical process research and development is recognised as a key function during the commercialisation of a new product particularly in the generic and contract manufacturing arms of the chemical, agrochemical and pharmaceutical industries.
The synthesis and individual processes must be economic, safe and must generate product that meets the necessary quality requirements.
This 2-day course presented by highly experienced process chemists will concentrate on the development and optimisation of efficient processes to target molecules with an emphasis on raw material cost, solvent choice, yield improvement, process efficiency and work up, and waste minimisation.
Process robustness testing and reaction optimisation via stastical methods will also be covered.
A discussion of patent issues and areas where engineering and technology can help reduce operating costs.
The use of engineering and technology solutions to reduce costs will be discussed and throughout the course the emphasis will be on minimising costs and maximising returns.
Conference 4-5 DEC 2014
TITLE . Organic Process Research & Development – India
Subtitle:The 32nd International Conference and Exhibition
When:04.12.2014 – 05.12.2014
Where:National Chemical Laboratory – Pune, India
Brochure:View Brochure
Register..http://scientificupdate.co.uk/conferences/conferences-and-workshops.html
for
- Process Research & Development Chemists
- Chemical Engineers in Industry
- Heads of Departments & Team Leaders
Benefits
- Invest in yourself: keeping up to date on current developments and future trends could mean greater job security.
- Learn from a wide range of industrial case studies given by hand-picked industrial speakers.
- Take home relevant ideas and information that are directly applicable to your own work with the full proceedings and a CD of the talks.
- Save time. Our intensive, commercial-free programme means less time away from work.
- Meet and network with the key people in the industry in a relaxed and informal atmosphere.
Do you want to improve efficiency and innovation in your synthetic route design, development and optimisation?
The efficient conversion of a chemical process into a process for manufacture on tonnage scale has always been of importance in the chemical and pharmaceutical industries. However, in the current economic and regulatory climate, it has become increasingly vital and challenging to do so efficiently. Indeed, it has never been so important to keep up to date with the latest developments in this dynamic field.
At this Organic Process Research & Development Conference, you will hear detailed presentations and case studies from top international chemists. The hand-picked programme of speakers has been put together specifically for an industrial audience. They will discuss the latest issues relating to synthetic route design, development and optimisation in the pharmaceutical, fine chemical and allied fields. Unlike other conferences, practically all our speakers are experts from industry, which means the ideas and information you take home will be directly applicable to your own work.
The smaller numbers at our conferences create a more intimate atmosphere. You will enjoy plenty of opportunities to meet and network with speakers and fellow attendees during the reception, sit-down lunches and extended coffee breaks in a relaxed and informal environment. Together, you can explore the different strategies and tactics evolving to meet today’s challenges.
This is held in Pune, close proximity to Mumbai city, very convenient to stay and travel to either in Pune or Mumbai. I feel this should be an opportunity to be grabbed before the conference is full and having no room
Hurry up rush
References
1 https://newdrugapprovals.org/scientificupdate-uk-on-a-roll/
2 http://scientificupdate.co.uk/conferences/conferences-and-workshops.html
3 http://en.wikipedia.org/wiki/Pune
PROFILES
Will Watson
Dr Will Watson gained his PhD in Organic Chemistry from the University of Leeds in 1980. He joined the BP Research Centre at Sunbury-on-Thames and spent five and a half years working as a research chemist on a variety of topics including catalytic dewaxing, residue upgrading, synthesis of novel oxygenates for use as gasoline supplements, surfactants for use as gasoline detergent additives and non-linear optical compounds.
In 1986 he joined Lancaster Synthesis and during the next 7 years he was responsible for laboratory scale production and process research and development to support Lancaster’s catalogue, semi-bulk and custom synthesis businesses.
In 1993 he was appointed to the position of Technical Director, responsible for all Production (Laboratory and Pilot Plant scale), Process Research and Development, Engineering and Quality Control. He helped set up and run the Lancaster Laboratories near Chennai, India and had technical responsibility for the former PCR laboratories at Gainesville, Florida.
He joined Scientific Update as Technical Director in May 2000. He has revised and rewritten the ‘Chemical Development and Scale Up in the Fine Chemical & Pharmaceutical Industries’ course and gives this course regularly around the world. He has been instrumental in setting up and developing new courses such as ‘Interfacing Chemistry with Patents’ and ‘Making and Using Fluoroorganic Molecules’.
He is also involved in an advisory capacity in setting up conferences and in the running of the events. He is active in the consultancy side of the business and sits on the Scientific Advisory Boards of various companies.
………………………………………………………………………………………………….
John Knight
Dr John Knight gained a first class honours degree in chemistry at the University of Southampton, UK. John remained at Southampton to study for his PhD in synthetic methodology utilizing radical cyclisation and dipolar cyloaddition chemistry.
After gaining his PhD, John moved to Columbia University, New York, USA where he worked as a NATO Postdoctoral Fellow with Professor Gilbert Stork. John returned to the UK in 1987 joining Glaxo Group Research (now GSK) as a medicinal chemist, where he remained for 4 years before moving to the process research and development department at Glaxo, where he remained for a further 3½ years.
During his time at Glaxo, John worked on a number of projects and gained considerable plant experience (pilot and manufacturing). In 1994 John moved to Oxford Asymmetry (later changing its name to Evotec and most recently to Aptuit) when it had just 25 staff. John’s major role when first at Oxford Asymmetry was to work with a consultant project manager to design, build and commission a small pilot plant, whilst in parallel developing the chemistry PRD effort at Oxford Asymmetry.
The plant was fully operational within 18 months, operating to a 24h/7d shift pattern. John continued to run the pilot plant for a further 3 years, during which time he had considerable input into the design of a second plant, which was completed and commissioned in 2000. After an 18-month period at a small pharmaceutical company, John returned to Oxford in 2000 (by now called Evotec) to head the PRD department. John remained in this position for 6.5 years, during which time he assisted in its expansion, established a team to perform polymorph and salt screening studies and established and maintained high standards of development expertise across the department.
John has managed the chemical development and transfer of numerous NCE’s into the plant for clients and been involved in process validations. He joined Scientific Update in January 2008 as Scientific Director.
Pune images
From top:1 Fergusson College, 2 Mahatma Gandhi Road, Shaniwarwada 3 the HSBC Global Technology India Headquarters, and the 4National War Memorial Southern Command
NCL PUNE
The National Chemical Laboratory is located in the state of Maharashtra in India. Maharashtra state is the largest contributor to India’s GDP. The National Chemical Laboratory is located in Pune city, and is the cultural capital of Maharashtra. Pune city is second only to Mumbai (the business capital of India) in size and industrial strength. Pune points of interest include: The tourist places in Pune include: Lal Deval Synagogue, Bund Garden, Osho Ashram, Shindyanchi Chhatri and Pataleshwar Cave Temple.
MAKE IN INDIA
http://makeinindia.com/sector/pharmaceuticals/
Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 
KEYWORDS
JOHN KNIGHT, WILL WATSON, SCIENTIFIC UPDATE, PROCESS, COURSE, CONFERENCE, INDIA, PUNE, PROCESS DEVELOPMENT, LOW COST, MANUFACTURING, SCALEUP
Glenmark’s TRPA1 antagonist ‘GRC 17536’ shows positive data in a proof of concept study
MUMBAI, India, Sep 17, 2014
- Glenmark's first in class TRPA1 antagonist, GRC 17536, has shown positive data in a Phase 2a proof of concept study in patients with painful diabetic neuropathy
Glenmark Pharmaceuticals today announced that its first in class Transient Receptor Potential Ankyrin 1 (TRPA1) antagonist, GRC 17536 has shown positive data in a Phase 2a double blind, placebo controlled, multi-centre, proof of concept study conducted on 138 patients in Europe and India.
A statistically significant and clinically relevant response was seen in a prospectively-identified, substantial sub-group of patients with moderate to severe pain who had relatively intact sensory responses as detected by a standardized testing methodology. GRC 17536 was well-tolerated with no evidence of CNS or other drug related side effects.
Patrick Keohane, Chief Medical Officer, Glenmark stated “Diabetic neuropathy remains a difficult to manage chronic clinical condition with limited therapeutic options. These initial efficacy and safety data with GRC 17536, a peripherally acting novel therapeutic, are encouraging, and Glenmark intends to be ready to file for a Phase 2b dose range finding study in patients with neuropathic pain before the end of this financial year. This announcement also reaffirms our position globally in the development of novel pain therapies”.
Commenting on this result, Dr. Michael Buschle, Chief Scientific Officer & President – Biologics, Glenmark Pharmaceuticals mentioned, “This is very promising and GRC 17536 may be useful for several indications which we will pursue”.
The Glenmark TRPA1 program includes indications in pain as well as respiratory. Inhaled doses of GRC 17536 are also being tested in a Phase 2A proof of concept study in patients with Chronic Cough.
Note on TRPA1
TRPA1 is an ion channel expressed on peripheral and spinal sensory neurons and it mediates pain signal transmission. It functions as a cellular sensor for detecting painful mechanical, biochemical and thermal stimuli that cause sensory nerve hyperactivity during chronic pathologies including chronic pain, inflammation, itch and cough. TRPA1 receptor is shown to induce pain hypersensitivity in animal models of diabetic neuropathic pain and its blockade attenuates pain hypersensitivity as well as later loss of the nerve fibers and their function. GRC 17536 is a potent, selective and first in class antagonist of TRPA1 receptor. Preclinical studies have demonstrated its effectiveness in animal models of neuropathic and inflammatory pain including the peripheral diabetic neuropathic pain, osteoarthritic pain, postoperative pain and chemotherapy induced pain which supports potential utility of TRPA1 blockade in therapeutic pain management.
About Glenmark Pharmaceuticals Ltd
Glenmark Pharmaceuticals Ltd. (GPL) is a research-driven, global, integrated pharmaceutical company and ranked among the top 80 Pharma & Biotech companies of the world in terms of revenues as per SCRIP 100 Rankings. Glenmark is a leading player in the discovery of new molecules both NCEs and NBEs. Glenmark has several molecules in various stages of clinical development and primarily focused in the areas of Inflammation, Pain and Oncology. The company has significant presence in branded formulations across emerging economies including India. Its subsidiary, Glenmark Generics Limited services the requirements of the US and Western Europe markets.
Hydrogenation in flow: homogenous and heterogeneous catalysts using Teflon AF-2400 to effect gas-liquid contact at elevated pressure
http://pubs.rsc.org/en/Content/ArticleLanding/2011/SC/c1sc00055a#!divAbstract
M. O’Brien, N. Taylor, A. Polyzos, I.R. Baxendale, S.V. Ley, Chem. Sci. 2011, 2, 1250-1257.
A Tube-in-Tube reactor/injector has been developed, based on a gas-permeable Teflon AF-2400 membrane, which allows both heterogeneous and homogeneous catalytic hydrogenation reactions to be efficiently carried out at elevated pressure in flow, thereby increasing the safety profile of these reactions. Measurements of the gas permeation through the tubing and uptake into solution, using both a burette method and a novel computer-assisted ‘bubble counting’ technique, indicate that permeation/dissolution follows Henry’s law and that saturation is achieved extremely rapidly. The same gas-permeable membrane has also been shown to efficiently effect removal of excess unreacted hydrogen, thus enabling further downstream reaction/processing.
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Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton† *
Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), Two Corporate Drive, South San Francisco, CA 94080, United States. E-mail: mattduncton@yahoo.com; Tel: +1 917-345-3183
First published on the web 22nd August 2011
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
The addition of a radical to a heteroaromatic base is commonly referred to as a Minsici reaction. Such reactions constitute a broad-set of selective CH-functionalization processes. This review describes some of the major applications of Minisci reactions and related processes to medicinal or biological chemistry, and highlights some potential developments within this area.
Introduction
The aim of this review is to summarize the use of Minisci reactions within medicinal chemistry, and to highlight some future opportunities to continue progression of this chemistry. As such, it is not an aim that detailed mechanistic information, or a comprehensive list of examples be described. For this, the reader is directed to excellent articles from Minisci, Harrowven and Bowman.1–3 Rather, the review is written to show that Minisci reactions are extremely valuable CH-functionalization processes within medicinal chemistry. However, their use has been somewhat under-utilized when compared with other well-known selective transformations (e.g. palladium-catalysed cross-couplings). Therefore, it is hoped that in the future, Minisci chemistry will continue to develop, such that the reactions become a staple-set of methods for medicinal and biological chemists alike.
To aid discussion, the review is divided in to several sections. First, some historical perspective is given. This is followed by a discussion of scope and limitations. The main-body of the review describes some specific examples of Minisci reactions and related processes, with a focus on their use within medicinal, or biological chemistry. Finally, brief mention is given to potential future applications, some of which may be beneficial in providing ‘high-content’ diverse libraries for screening.
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
http://pubs.rsc.org/en/content/articlehtml/2011/md/c1md00134e
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WIKI
The Minisci reaction is a named reaction in organic chemistry. It is a radical substitution to an aromatic compound, in particular to a heteroaromatic base, that introduces an alkyl group. The reaction was published about in 1971 by F. Minisci.[1] The aromatic compound is generally electron-deficient and with N-aromatic compounds the nitrogen atom is protonated.[2] A typical reaction is that between pyridine and pivalic acid to 2-tert-butylpyridine with silver nitrate, sulfuric acid and ammonium persulfate. The reaction resembles Friedel-Crafts alkylation but with opposite reactivity and selectivity.[3]
The Minisci reaction proceeds regioselectively and enables the introduction of a wide range of alkyl groups.[4] A side-reaction is acylation.[5] The ratio between alkylation and acylation depends on the substrate and the reaction conditions. Due to the simple raw materials and the simple reaction conditions the reaction has many applications in heterocyclic chemistry.[6][7]
Mechanism
A free radical is formed from the carboxylic acid in an oxidative decarboxylation with silver salts and an oxidizing agent. The oxidizing agent reoxidizes the silver salt. The radical then reacts with the aromatic compound. The ultimate product is formed by rearomatisation. The acylated product is formed from the acyl radical.[4][5]
References
- F. Minisci, R. Bernardi, F. Bertini, R. Galli, M. Perchinummo: Nucleophilic character of alkyl radicals—VI : A new convenient selective alkylation of heteroaromatic bases, in: Tetrahedron 1971, 27, 3575–3579.
- Minisci reaction Jie Jack Li in Name Reactions 2009, 361-362, doi:10.1007/978-3-642-01053-8_163
- Strategic applications of named reactions in organic synthesis: background and detailed mechanisms László Kürti, Barbara Czakó 2005
- F. Fontana, F. Minisci, M. C. N. Barbosa, E. Vismara: Homolytic acylation of protonated pyridines and pyrazines with α-keto acids: the problem of monoacylation, in: J. Org. Chem. 1991, 56, 2866–2869; doi:10.1021/jo00008a050.
- M.-L. Bennasar, T. Roca, R. Griera, J. Bosch: Generation and Intermolecular Reactions of 2-Indolylacyl Radicals, in: Org. Lett. 2001, 3, 1697–1700; doi:10.1021/ol0100576.
- P. B. Palde, B. R. McNaughton, N. T. Ross, P. C. Gareiss, C. R. Mace, R. C. Spitale, B. L. Miller: Single-Step Synthesis of Functional Organic Receptors via a Tridirectional Minisci Reaction, in: Synthesis 2007, 15, 2287–2290; doi:10.1055/s-2007-983792.
- J. A. Joules, K. Mills: Heterocyclic Chemistry, 5. Auflage, S. 125–141, Blackwell Publishing, Chichester, 2010, ISBN 978-1-4051-9365-8.
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4-methoxyphenyl methanol, (4-メトキシフェニル)メタノール NMR, IR , MASS
(4-methoxyphenyl)methanol
IUPAC Name: 4-methoxyphenyl methanol
C6H10O3; MW = 138.17
The molecule contains two oxygens, and from the analysis, contains four double bonds, carbonyls or rings. The large number of degrees of unsaturation strongly suggests an aromatic compound (DU = 4).
The mass spectrum displays a molecular ion, which is the base peak, an m-1 and an m-17, all of which are consistent with a simple alcohol.
The 13C spectrum contains six peaks, indicating that the molecule has some elements of symmetry. The quartet at 
56 and the triplet at 71 represent a CH3 and a CH2 group which are deshielded by electronegative atoms (most likely oxygen); the peaks at 161 – 128 are in the aromatic region; the fact that two doublets and two singlets are observed strongly suggests 1,4-disubstitution.
The proton NMR also shows evidence for aromatic 1,4-disubstitution and suggests that the methyl and methylene are isolated and adjacent to electronegative groups. A peak consistent with an alcoholic OH can also be seen.
The IR is consistent with an aromatic alcohol containing no carbonyl group, suggesting that the second oxygen is involved in an ether linkage.
The simplest structure which is consistent with all of these data would be an aromatic compound containing an alcohol group and a methyl ether, situated 1,4 relative to each other.
IH NMR
The proton NMR has two doublets at 6.9, consistent with aromatic 1,4-disubstitution, and three singlets, areas 3, 2 and 1. The singlets at 3.6 and 4.7 are highly shifted and suggest isolated CH3 and CH2 groups adjacent to one or more electronegative atoms or groups. The singlet, area 1, would be consistent with an alcohol.
13C NMR
The 13C spectrum contains six peaks, indicating that the molecule has some elements of symmetry. The quartet at 56 and the triplet at 71 represent a CH3 and a CH2 group which are deshielded by electronegative atoms (most likely oxygen); the peaks at 161 – 128 are in the aromatic region; the fact that two doublets and two singlets are observed strongly suggests 1,4-disubstitution.
13C NMR Data: q-56.0; t-71.0; d-114.3; d-128.3; s-160.9; s-133.2
13C NMR Assignments: 
MASS
The mass spectrum consists of a molecular ion at 138, which is also the base peak, an m-1 peak at 137, indicating the presence of a labile hydrogen (OH or CHO), and an m-17 peak (loss of HO-). The spectrum is consistent with an alcohol which cannot readily break down to form other stable radical cations.
Mass Spectrum Fragments: 
IR
3400-3200 cm–1: strong OH peak 3100 cm–1: small peak, suggesting possible unsaturated CH 2900 cm–1: strong peak suggesting saturated CH 2200 cm–1: no unsymmetrical triple bonds 1710 cm–1: no carbonyl 1610 and 1500 cm–1: sharp peaks, consistent with aromatic carbon-carbon double bonds
Synthetic Communications, 18, p. 613, 1988 DOI: 10.1080/00397918808064019
Synthesis, p. 1081, 1984
Tetrahedron Letters, 32, p. 3243, 1991
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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 GLENMARK- GENERICS LTD, Research centre as 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 25 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
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