Process for the solid state synthesis of enantiopure B-aminoalcohols from racemic epoxides

摘要

The invention relates to a process for the solid state synthesis of enantiopure beta-aminoalcohols by preparing inclusion complexes of aryloxyepoxide with cyclodextrin by adding an epoxide in equimolar ratio in an organic solvent to an aqueous solution of cyclodextrin, reacting the cyclodextrin complex of aryloxyepoxide with a nucleophile in solid state by intimately grinding the mixture using a mortar and pestle, continuing the mixing till the starting epoxide disappeared on tic, removing excess amines under vacuum, extracting the beta-aminoalcohols produced with a solvent with yields of more than 50% and enantioselectivity of upto 100%.