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 (+)-(S)-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.
Convenient lipase-assisted preparation of both enantiomers of suprofen, a non-steroidal anti-inflammatory drug
Nicolosi Giovanni;Patti A;
1996
Abstract
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 (+)-(S)-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.File in questo prodotto:
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