TAXANE SYNTHESIS INTERMEDIATES AND METHODS OF PREPARATION THEREOF Russian patent published in 2000 - IPC

FIELD: organic synthesis. SUBSTANCE: in a method of preparing taxane side chain precursors, cis-beta-arylglycidate derivative having general formula I: (I) with (2R,3S) configuration is converted. In formula I, Ar is aryl and R hydrocarbon radical, preferably linear or branched alkyl optionally substituted by one or several alkyl radicals, so that could be possible regio- and stereospecific single-step preparation of beta-N- alkylamide and alpha-hydroxyl or their cyclic precursors according to Ritter reaction. Direct synthesis of linear chain is accomplished by bringing cis-beta-arylglycidate derivative I into reaction with nitrile R₂- CN (R₂ is aryl radical) in presence of protonic acid and water to form beta-arylisoserine derivative IIa: (IIa). Invention also relates to oxazolidine and oxazolidinone derivatives and novel baccatin derivatives. EFFECT: simplified procedure. 28 cl, 29 ex