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Synfacts 2011(7): 0702-0702  
DOI: 10.1055/s-0030-1260482
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of the COX-2 Inhibitor GW406381X

Contributor(s): Philip Kocienski
M. C. Wilkinson*
GlaxoSmithKline, Stevenage, UK
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Publication History

Publication Date:
17 June 2011 (online)

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Significance

A new metal- and halogen-free variant of the Friedel-Crafts acylation using carboxylic acid substrates is promoted by methanesulfonic anhydride (1.3 equivalent) and as little as 1.3 equivalent of the arene. In general, no additional solvent is required making the reaction very atom-efficient. The methanesulfonic acid waste stream is biodegradable.