| Propylene Carbonate as a Replacement for Dichloroethane in Hydroacylation Reactions |
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Trevor Laird
Hydroacylation, the addition of an aldehyde across a double or triple bond to give a ketone is an atom efficient transformation catalysed by a variety of transition metals. Intramolecularly it is very efficient, but the intermolecular reaction is plagued by a side reaction, namely the decarbonylation of the aldehyde, unless the aldehyde contains a group which can chelate to the transition metal catalyst.
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| New Protecting Group; Di-tert-butylisobutylsilyl (BIBS) |
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Trevor Laird
Although process chemists try to avoid using protecting groups, occasionally they have to be used in the manufacture of complex multifunctional molecules. The books by Wuts and Greene (Protecting Groups in Organic Synthesis, 4th Ed, Wiley-Interscience, NY, 2007) and Kocienski (Protecting Groups, 3rd Ed, Thieme Stuttgart, 2005) are very useful compilations of the types of groups, and methods for their attachment and removal.
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| Metal and Chloride Free Friedel-Crafts Acylation |
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Dr Will Watson
This modification of the classical Friedel-Crafts acylation reaction still uses a stoichiometric amount of catalyst and generates the expected mixture of ortho and para substituted products, but it has the advantage that a carboxylic acid is used as the acylating component ...
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| Heck Couplings with In Situ Generated Diazonium Salts |
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Dr Will Watson
The Heck-Matsuda coupling involves the generation of a diazonium salt which is then coupled with an olefin. In this paper, the reaction is run with a sub-stoichiometric amount of methanesulphonic acid (10-20mol%) in methanol which limits the amount of diazonium salt that can be present at any one time during the reaction.
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| Weinreb Amide Chemistry |
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Dr John Knight
At our recent Organic Process Research and Development conference (Budapest) we were treated to a number of excellent talks, one of which was given by Olivier Dirat (Pfizer). The presentation featured some chemistry using a Weinreb amide and proposed a mechanism that could explain the formation of the N-methylamide impurity.
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| Nitromethane Chemistry |
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Dr John Knight
Over the past few years I have noticed resurgence in the use of nitrocompounds, in academic papers at least, especially in combination with organocatalysis as a powerful means of forming C-C bonds enantioselectively.
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| Book Review |
| Pharmaceutical Process Development, Current Chemical and Engineering Challenges |
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RSC Publishing, 2011 (ISBN 978-1-84973-146-1)
This book, edited by John Blacker and Mike Williams, explores how advances in synthetic organic chemistry, process technology and chemical engineering have impacted on the manufacture of pharmaceuticals. It covers diverse subjects such as route design and selection, the interface with medicinal chemistry, the importance of green chemistry, the design of safe chemical reactions, the crucial role of physical organic chemistry in understanding chemical processes, the role of the analyst, reactor design, purification and separation, and solid state chemistry and its role in formulation. The book is aimed at graduates and postgraduates seeking a career in the industry and at chemists and chemical engineers already working with pharmaceuticals. |
| ... and finally - you might be an engineer if...... |
| ... you've tried to repair a £5 radio. |
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Dates for your diary...
Click to view our 2011 & 2012
Conference and Course Dates
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CONFERENCES
Developing Chemical Processes for Active Pharmaceutical Ingredients (APIs)
6 & 7 February 2012
Mumbai, India
Organic Process Research & Development
19 - 21 March 2012
San Francisco, CA, USA
Modern Synthetic Methods and Chiral Europe
14 - 16 May 2012
Prague, Czech Republic
COURSES
Biocatalysis as Tool for the Synthetic Chemist
1 & 2 December 2011
Sussex, UK
Scaling from Milligrams to
1-2kg
8 & 9 February 2012
Mumbai, India
Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries
8 - 10 February 2012
Mumbai, India
Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries
6 - 8 March 2012
Florence, Italy
Understanding Polymorphism & Crystallisation Issues in the Pharmaceutical Industry
14 - 16 March 2012
Lison, Portugal
Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries
14 - 16 March 2012
San Francisco, CA, USA
Interfacing Chemistry with Patents
20 & 21 March 2012
Barcelona, Spain
Heterogeneous Catalytic Hydrogenation
16 & 17 April 2012
Brussels, Belgium
Scaling from Milligrams to
1-2kg
18 & 19 April 2012
Brussels, Belgium
Practical Approaches to Quality by Design for Pharmaceutical Process R&D and Manufacturing
24 - 26 April 2012
Clearwater Beach, FLA, USA
Medicinal Chemistry
25 - 27 April 2012
Edinburgh, Scotland
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