O-ALKYL MACROLIDE AND AZALIDE DERIVATIVES AND REGIOSELECTIVE PROCESS FOR THEIR PREPARATION

摘要

The present invention relates to a process for regioselective O-alkylation of macrolide and azalide derivatives, specifically 11-0-alkyl derivatives represented by formula (I) (1) R<1> wherein A is 14-membered macrolide derivative and 15-membered azalide derivative, and R<1> is C1-C4 alkyl group comprising reacting an macrolide or azalide derivative with vicinal hydroxyl system with diazoalkane of the formula R<2> - CH N2 wherein R<2> is a hydrogen or C1-C3 alkyl group in the presence of transition-metal halides and of boric acid as catalysts, respectively, preferably H3B03, TiC14 and SnC12 in suitable inert organic solvent and to new compounds represented by the formula (I). C