Patent ID: 6239313
Filing Date: 2001-05-29
Classification: C07B,C07C,C07D

Abstract:
A process for the solid state synthesis of enantiopure .beta.-aminoalcohols having the formula ##STR8##wherein R is alkyl, halo, or alkoxy group, and R' and R"" is alkyl or cycloalkyl, from racemic epoxides which comprises:(a) preparing inclusion complexes of aryloxyepoxide with cyclodextrin by adding an epoxide in equimolar ratio in an organic solvent to an aqueous solution of cyclodextrin at a temperature ranging between 30-80.degree. C.;(b) reacting the cyclodextrin complex of aryloxyepoxide with a nucleophile in solid state by intimately grinding the mixture using a mortar and pestle;(c) continuing the mixing till the starting epoxide disappeared on tlc within a period ranging between 3-12 hours;(d) removing excess amines under vacuum;(e) extracting the .beta.-aminoalcohols with a solvent with yields of more than 50% and enantioselectivity of up to 100%.