Method of preparing optically active cyanohydrin derivatives and their conversion products, and optically active compounds to be obtained in this manner.

摘要

The invention relates to a method of preparing optically active alcohols of formula 4 <CHEM> wherein R is a monocyclic or bicyclic aryl or heteroaryl group substituted with one or more groups X, wherein X is a hydroxy, alkoxy(1-5C), alkyl(1-5C)carbonyloxy, amino, alkyl(1-5C)carbonylamino, alkyl(1-5C)sulphonylamino, nitro, alkyl(1-5C)sulphonyl, alkyl(1-5C)carbonyl, halogen, cyano, alkyl(1-5C), cycloalkyl(5-12C), or a cyclic group annelated with the aryl group or heteroaryl group, or wherein R is a saturated or unsaturated straight or branched alkyl group having 1-30 C-atoms which may be substituted with halogen, alkoxy(1-5C), alkylthio(1-5C), phenyl or phenoxy optionally substituted with one or more groups X, and A is a radical obtained by derivation of the cyano group, by protecting the hydroxy group of an optically active cyanohydrin, converting the cyano group of the protected cyanohydrin into a desired group, and deprotecting the hydroxy group. The method according to the invention is suitable for the preparation of optically pure cyanohydrin derivatives which may be pharmacologically active compounds, or form suitable starting compounds for the preparation of optically pure biologically active products.