PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE 3-AMINO-2 -HYDROXYPROPIONIC CYCLOPROPYLAMIDE DERIVATIVES AND SALTS THEREOF

摘要

The invention aims at providing an industrially practical process by which optically active 3-amino-2-hydroxypropionic cyclopropylamide derivatives useful as intermediates of drugs or salts thereof can be easily produced from inexpensive and easily available raw materials; and these useful intermediates. This aim can be attained by a process which comprises subjecting an easily available 2-halo-3-oxopropionic acid derivative to asymmetric reduction and epoxidation successively to form an optically active epoxycarboxylic acid derivative, reacting the epoxycarboxylic acid derivative with cyclopropylamine to form an optically active epoxyamide derivative, reacting the epoxyamide derivative with nitrile to form an optically active oxazoline-amide derivative, and subjecting the oxazoline-amide derivative to selective acidic solvolysis of oxazoline skeleton to form an optically active 3-amino-2-hydroxypropionic cyclopropylamide derivative or a salt thereof.