SYNTHESIS OF PRECURSORS OF 13-ALKYL EPOTHILONE DERIVATIVES BY ANTIBODY-CATALYZED RETROALDOL REACTION

摘要

The invention relates to novel 13-lower alkyl epothilones of formula (IA); wherein R1 is methyl, hydroxymethyl, halomethyl, methylthio or methoxy; R2 is hydrogen or methyl, R3 is lower alkyl, and Z is O or a bond; intermediates and a process for the preparation of such 13-lower alkyl epothilones and epothilones in general; a pharmaceutical composition comprising such 13-lower alkyl epothilones and the use of such compounds for the treatment of tumor diseases; a method of treatment of warm-blooded animals; catalytic antibodies having aldolase activity and a process for enantioselectively resolving a racemic mixture of aldol synthons by means of antibody catalyzed retro-aldol reaction.