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

机译:由外消旋环氧化物固态合成对映体纯的B-氨基醇的方法

摘要

The invention relates to a process for the solid state synthesis of enantiopure &bgr;-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 &bgr;-aminoalcohols produced with a solvent with yields of more than 50% and enantioselectivity of upto 100%.
机译:本发明涉及对映体纯的氨基醇的固态合成方法,该方法是通过在有机溶剂中向环糊精的水溶液中加入等摩尔比的环氧化物,制备芳氧基环氧化物与环糊精的包合配合物,使芳氧基环氧化物的环糊精配合物与通过使用研钵和研棒对混合物进行紧密研磨来使其成为固态亲核试剂,继续混合直至tic上的起始环氧化物消失,在真空下除去过量的胺,然后萃取溶剂产生的&-bgr;-氨基醇的收率超过50%对映选择性高达100%。

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