Issue 27 December 2008

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Chiral Switches and Patentability
In the 1990s it was the fashion to change from racemic drugs to single enantiomers with some notable marketing successes being Esomeprazole Escitalopram, Dexketoprofen and Levobupivicaine. These drugs were originally marketed as racemates and then a “chiral switch” to single enantiomer was carried out, the marketing emphasis being on improvement in desired drug characteristics (potency, efficiency, safety etc). Patentability was also important.
What Temperature is Required for the Generation of Metallated Aromatic Substrates?
Metallation of aromatic compounds either via DoM or by metal-halogen exchange is usually carried out at cryogenic temperatures and if there is a carbonyl or nitrile in the molecule temperatures down to -100°C are usually required. However 2 recent publications have started to challenge this requirement and/or find alternative methodology to get to the same intermediate without the cryogenic requirement.
Rhodium Catalysed Direct Arylation of Pyridines and Quinolines
Pyridines are often difficult to functionalise, particularly by aryl groups and often a “de novo” synthesis may be required when cross-coupling methods fail.
Transformation of Triazoles into Imidazoles
1,2,3-Triazoles are easily made by addition of azides to olefins but their further transformation to other useful compounds is not always possible.
Addition of CO2 to Styrenes
The Ideal Combination: Viagra® and Aspirin?
Oseltamivir – Yet Another Academic Synthesis Reported
Book Review

The Chemistry of Organomagnesium Compounds Parts 1-2: R-Mg
... and finally ...
... you know you've been in the lab too long when ... the Christmas night out reveals scientists can't dance, although a formula for the movement of hands and feet combined with beats per min is found scrawled on a napkin by a waiter the next day.
Dates for your diary...
Our NEW 2009 Conference and Course Dates are now available!

CONFERENCES
Process Analytical Technologies (PAT)
17 - 18 Mar 2009
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Polymorphism & Crystallization
19 - 20 Mar 2009
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Organic Process Research and Development
27 - 30 Apr 2009
Fort Lauderdale, FLA, USA
COURSES
Chemical Development & Scale-Up in the Fine Chemical & Pharmaceutical Industries
16 - 18 Feb 2009
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03 - 05 Mar 2009
Rome, Italy
Medicinal Chemistry
25 - 27 Feb 2009
Brussels, Belgium
Advanced Aromatic Heterocyclic Chemistry
11 - 13 Mar 2009
Basel, Switzerland
Effective Information Retrieval
17 - 18 Mar 2009
London, UK
Secrets of Batch Process Scale-Up
18 - 20 Mar 2009
San Diego, CA, USA

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