发明申请
US20110178305A1 PROCESS FOR THE PREPARATION OF 3,4-EPOXY-2-AMINO-1-SUBSTITUTED BUTANE DERIVATIVES AND INTERMEDIATE COMPOUNDS THEREOF 审中-公开
制备3,4-环氧-2-氨基-1-取代的丁烷衍生物及其中间体化合物的方法

PROCESS FOR THE PREPARATION OF 3,4-EPOXY-2-AMINO-1-SUBSTITUTED BUTANE DERIVATIVES AND INTERMEDIATE COMPOUNDS THEREOF
摘要:
The present invention relates to a process for the preparation of threo-3,4-epoxy-2-amino-1-substituted butane derivatives represented by general Formula I which comprises reacting compound of Formula III or salt thereof with an active ester of acid of Formula IV and treating the product thereof with base. The carbon atom bonded to the radical R3 in Formula I and IV is in the (R)-, (S)- or (R,S)-configuration. The compounds of Formula I and III, particularly in their (2S,3R) configuration are useful intermediates for the preparation of atazanavir bisulfate.
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