Patent ID: 6593115
Filing Date: 2003-07-15
Classification: C07D,C12P

Abstract:
A process for preparing a compound of formula I: wherein:X is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl and substituted aryl; R1 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, and heterocyclo; and P1 and P2 are independently selected from the group consisting of hydrogen, aralkyl, substituted aralkyl, trialkylsilyl, triarylsilyl, dialkylarylsilyl, diarylalkylsilylalkoxyalkyl, and aralkyloxyalkyl; comprising treating an epothilone compound of formula III or formula IV: wherein:R1 is as defined above; R2 is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, heterocyclo or â€ƒand R3 and R4 are selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl and heterocyclo; with an enzyme selected from the group consisting of chymotrypsin, pancreatin, and an esterase capable of cleaving or degrading said compound to form a compound of formula VI: wherein R1 and R2 are as defined above; optionally esterifying the carboxyl group of said compound; optionally reacting the resulting esterified compound to form protecting groups on the hydroxyl groups of said compound; and reacting the resulting compound with a suitable oxidizing agent to form said compound of formula I.