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Issue 41 January/February 2012

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What's New in Process Chemistry?
Newsletter Issue 41 January/February 2012.
Scientific Updates' What's New in Process ChemistryScientific Update
What's New in Process Chemistry.
Monoalkylation of Acetonitrile by Primary Alcohols

Trevor Laird
The group of Cossy at CNRS, Paris in collaboration with the process development groups at Sanofi Aventis (Sisteron) has discovered a way to react primary alcohols with acetonitrile to produces extended nitriles in a very atom efficient reaction. (Org Lett, 2011, 13(15), 4084-7).

A Simple N-Formylation Procedure

Trevor Laird
A simple procedure for formylating a wide variety of amino-acid esters and primary amines has been discovered by a group at London (Western Ontario, Canada).

From Malonic Acid to Amide, Ester, or β-Ketoester

Dr Will Watson
In this paper from Pfizer, malonic acids are reacted with carbonyl diimidazole at room temperature to generate an intermediate mono-acid imidazole which can be reacted with amines (10 examples, 85-100% yield with one failure - 1,1-cyclopropanedicarboxylic acid). 

Direct N-alkylation of Amines with Alcohols

Dr John Knight
In recent years there have been a number of groups publish on the direct alkylation of amines using alcohols using a range of transition metal catalysts (eg Ru, Cu, Ir).

The Impact of Lithium Salts

Dr John Knight
In an interesting article, Hevia and Mulvey (Angew Chem Int Ed, 2011, 50, (29), 6448) discuss the impact lithium salts have on organometallic chemistry, making the point that even very small amounts of lithium chloride can have dramatic effects on the chemistry. 

Book Review
Fine Chemicals; the Industry and the Business

2nd Edition, Wiley 2011 (ISBN 078-0-470-62767-9.)

This unique book, by Peter Pollak, who worked for Lonza in Switzerland and USA for over 30 years in a variety of roles including process development, takes a comprehensive view of the products, markets and technology of the fine chemical industry. Part 1 covers the types of fine chemical companies, the range of products and services, the role of R&D, particularly process R&D, technologies used and the challenges facing management. Part 2 covers the industries (pharma, agrochemical and animal health) and their markets, including issues such as pricing, distribution channels, IP, business development and promotion. Part 3 covers the outlook and examines issues such as globalisation, outsourcing and the future, with a particular emphasis on India and China.

The second edition has been substantially revised from the 2005 edition with lots of new, up-to-date figures.

Anyone working in the fine chemical industry needs to read this book which is highly recommended. The only negative is the large number of typos in the book.

... and finally ......
... A chemist walks into a pharmacy and asks the pharmacist,
"Do you have any acetylsalicylic acid?"
"You mean aspirin?" asked the pharmacist.
"That's it, I can never remember that word."
Don't Forget
if you have a useful, novel or new methodology, please This e-mail address is being protected from spambots. You need JavaScript enabled to view it , to share this with our extensive international network of organic process chemists (sent to over 15,000 readers!)

Dates for your diary...
Click to view our 2011 & 2012
Conference and Course Dates

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
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


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