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Convenient lipase-assisted preparation of both enantiomers of suprofen, a non-steroidal anti-inflammatory drug

✍ Scribed by Patrizia Mertoli; Giovanni Nicolosi; Angela Patti; Mario Piattelli

Publisher: John Wiley and Sons
Year: 1996
Tongue: English
Weight: 396 KB
Volume: 8
Category: Article
ISSN: 0899-0042
DOI: 10.1002/(sici)1520-636x(1996)8:5<377::aid-chir4>3.0.co;2-b

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✦ Synopsis

The resolution of rac-suprofen (1) catalysed by lipase in organic solvents was investigated. Direct esterification of rac-1 with methanol in dichorometane catalysed by Novozym@ 435 furnished the pharmacologically active (+)-Q-suprofen as unreacted product with excellent enantiomeric excess. The same procedure in toluene using Mucor miehei lipase adsorbed in Celite as catalyst afforded (-)-(R)-suprofen with good optical purity.