专利号:US-6239313-B1 优先权日:2000-02-16 标 题 :Process for the solid state synthesis of enantiopure B-aminoalcohols from racemic epoxides 发明人:KAKULAPATI RAMA RAO; NANDURI BHANUMATHI; ELETI RAJENDER REDDY 权利人:COUNCIL SCIENT IND RES 摘要:The invention relates to a process for the solid state synthesis of enantiopure β-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 β-aminoalcohols produced with a solvent with yields of more than 50% and enantioselectivity of upto 100%.
参考文献:10.1021/jm00119a011 摘要:Mauleón D, Pujol MD, Rosell G. Synthesis and beta-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols. J Med Chem. 1988 Nov;31(11):2122–6. doi: 10.1021/jm00119a011.