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What’s New in Process Chemistry – Issue 63 September 2018
A Kinetic Kick-Start: Deutetrabenazine (AustedoTM)- the First FDA Approved Deuterated Drug

A new paradigm in drug development began in the spring of last year with the Food and Drug Administration’s (FDA’s) approval of Teva pharmaceuticals’ VMAT2 inhibitor deutetrabenazine as a new chemical entity (NCE) under its 501(b)(2) legislation. This molecule is unique in that it is the first deuterium-substituted drug to reach the market and heralds

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Oiling the cogs- Practical tips, useful facts and resources: Organometallic highlight:

The generation of lithium-alkoxide based aryl and heteroaryl Grignard reagents by Mg-Br/Cl exchange in toluene- increased reactivity and wide applicability. Organomagnesium-based organometallics are used extensively in organic chemistry.[1] Historically the reagents were prepared by direct insertion of magnesium metal into organic halides. With demand for more industrially applicable methods, halogen-magnesium exchange using alkyl magnesium halides

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Reagent of the month: Lithium Aluminium hydride

One might think that this hard-hitting, students best friend (it will reduce just about anything given the right conditions and is the go-to reducing agent for exam questions involving a reduction) has little more to offer to the practising chemist. However, a recent paper by Harder etal (Angew Chem Int Ed. 2018, 57(24), 7156) demonstrates

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PTC – Tip of the Month – August 2018

  A patent issued this month cites the use of catalytic tetrabutylammonium bromide (TBAB) in the ring opening esterification of glycidyl ethers using acrylic acid and methacrylic acid (see Example 7). In PTC esterifications, we typically expect the presence of a base to form the carboxylate salt from the acid then the quat acrylate would

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Chromatographic Processes

Preparative chromatography is a versatile purification technique used in various industrial sectors including petrochemistry, sugar production, pharmaceutical and fine chemistry, to name only a few. While this technology is often considered complex, expensive and sometimes not scaleable, industrial success stories prove the opposite. In our recent webinar, Dr. Pfister from Ypso-Facto presented a reliable approach

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Recent Progress in Decarboxylative Oxidative Cross Coupling

A short review article, also from the group of Igor Larrosa at Manchester, on the use of aromatic carboxylic acids as coupling partners in biaryl synthesis, appeared earlier in European Journal of Organic Chemistry (2017, 3517-3527). It is suggested in the micro-review that benzoic acid derivatives are atom-economic alternatives to traditional cross  coupling partners, and

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Transition-Metal-Free Decarboxylative Bromination of Aromatic Carboxylic Acids

The brominative decarboxylation  reaction was demonstrated over a hundred and fifty years ago by Borodin (the famous composer, whose day job was as Professor of Organic Chemistry) and later developed by Hunsdiecker, whose name the reaction now bears. From an industrial viewpoint the transformation would be useful but the need to have a stoichiometric silver

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Utilization of fluoroform for difluoromethylation in continuous flow: a concise synthesis of α-difluoromethyl-amino acids

Published in Green Chemistry in 2018 C. Oliver Kappe is our tutor on our Flow Chemistry course and this abstract was published in Green Chemistry showing a collaboration with Lonza in making an API in flow. Abstract: Fluoroform (CHF3) can be considered as an ideal reagent for difluoromethylation reactions. However, due to the low reactivity

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Photo-Redox Catalysis

If you had suggested 10 years ago that it would be a good idea to try and develop some of the reactions that you can now carry out using photoredox catalysis, you would probably have been labelled as deluded, if you were not locked away for your own safety.  But photoredox catalysis has come a

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New Award for Women in Chemistry

I am delighted to share with you the announcement of a new award and a ‘call for nominations’. The ‘1st Dr Margaret Faul Women in Chemistry Award‘ is intended to recognize and highlight outstanding contributions by young women to research in organic chemistry. The prize provided by Thieme includes an award of € 5,000. For more

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Organic Process Research and Development
29 October 2018 -
31 October 2018

5th Winter Process Chemistry Conference & Exhibition
11 December 2018 -
13 December 2018

14th Winter Conference on Medicinal & Bioorganic Chemistry
27 January 2019 -
31 January 2019

Flow Chemistry and Continuous Processes Conference
08 April 2019 -
09 April 2019

Polymorphism and Crystallization Conference
08 April 2019 -
09 April 2019

Secrets of Batch Process Scale-Up
02 October 2018 -
04 October 2018

Industrial Phase-Transfer Catalysis
02 October 2018 -
03 October 2018

Safety & Selectivity in the Scale-Up of Chemical Reactions
09 October 2018 -
10 October 2018

Biocatalysis as a Tool for the Synthetic Chemist
11 October 2018 -
12 October 2018

Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries
15 October 2018 -
17 October 2018

New Perspectives on Flow Chemistry
03 October 2018
Preclinical Safety Assessment and Mitigation Strategies in Drug Discovery – Focus on Drug-Induced Liver Injury (DILI)
17 October 2018
Test Process Mixing Sensitivities Using the “Bourne Protocol”
13 November 2018
Deuterium in Organic Chemistry and Drug Discovery
14 November 2018
Speeding Drug Development through State-of-the-Art Impurity Control Strategies
15 November 2018
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