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Newsletter Issue 56 June/July 2015

Scientific Updates' What's New in Process ChemistryScientific Update
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Appearing and Disappearing Polymorphs

Dr Trevor Laird

Dr Trevor Laird (Scientific Update) talked about appearing and disappearing polymorphs and other solid forms in process development, during the '2nd Winter Process Chemistry' Conference in December. This involved a number of case studies including axitinib, Pfizer's anti-cancer drug, has 5 anhydrous forms and over 70 different solvates known to date and requires a complex crystallisation wash procedure to obtain the correct form. In another example from Merck-Schering Plough batches from one reactor train started to fail because of a yellow colouration. Product from an older reactor train did not have this problem. Temperature and humidity, particularly during drying were found to be critical. During drying a new anhydrate was being formed which then formed a new hydrate when exposed to moist air. The new hydrate is unstable forming the yellow impurity. The problem was solved by a modified wash and drying sequence.

Biocatalytic Cascade Syntheses

Dr Will Watson

Professor Nick Turner (University of Manchester) was the keynote speaker on the topic of biocatalysis, which was the special topic for the conference. The presentation covered a variety of new developments in the area of biocatalysis as well as highlighting the improvements that have taken place over the last 10-15 years. The final part of the talk covered biocatalytic cascade reactions where two or more enzymes are used in conjunction for example taking a 1,4-diketone and reacting it with an –transaminase and a monoamine oxidase and NH3:BH3, to produce enantiomerically pure pyrrolidines as shown below:


Iridium Catalysed Allylic Substitution Reactions with Carbon Nucleophiles

Dr Will Watson

Professor Erick Carreira (ETH, Zurich) presented work on iridium catalysed allylic substitution reactions with carbon nucleophiles using catalyst (1) during the '2nd Winter Process Chemistry' Conference in Manchester, in December 2014.



Challenges to Find Commercially Viable Routes to Agrochemicals

Dr Will Watson

Dr Roland Goetz (BASF) gave a presentation, during the 'Organic Process R & D' Conference in Pune in December which highlighted the challenges faced in trying to identify commercially viable routes to agrochemicals, which are typically low cost products that still contain a significant degree of complexity. One point he made was that companies have to re-register products every 10 years and as a result about 70% of old active ingredients have been withdrawn, mainly due to their negative impact on the environment.

Roland Scheme


API Synthesis using Transition Metal Catalysts

Dr Will Watson

Dr E.R.R. Chandreshekar (Dr Reddy's) discussed the use of transition metal catalysed reactions in the synthesis of API's during his presentation at the 32nd 'Organic Process R & D' Conference, held in Pune in December. The talk included a number of case studies including esomeprazole magnesium, cinacelet HCl, and sertraline HCl.

Dr Reddy scheme


The First 10 Lessons Learned in DoE

Today Quality by Design (QbD) is implemented primarily for economic considerations, and less because of possible regulatory flexibility that could be gained. The value added by QbD methodology has two components:
(i) very low cost of poor quality, and
(ii) systematically generated process understanding
(as Dr. Thien from Merck recently commented about the role of chemical process R&D: "...we make material ....and we make knowledge...").



Book Review; Biocatalysis in Organic Synthesis

Dr Trevor Laird

Book Review; Biocatalysis in Organic Synthesis, 3 volumes (Science Of Synthesis series); Thieme, 2014, ed K. Faber, W-D. Fessner and N.J.Turner

For organic chemists wanting to find out more about biotransformations in organic synthesis, this latest volume in the Science of Synthesis series is just the job. Nearly 2000 pages, written with the organic chemists in mind and with detailed practical procedures in each chapter showing how to perform the biotransformations.

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25 - 26 November 2015

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