The present invention provides an industrial process for effectively and advantageously preparing optically active 1-substituted amino-2,3-epoxypropanes useful as intermediates for preparing agricultural chemicals and medical products from optically active 1-substituted amino-2,3-propanediols used as raw materials. The present invention also provides useful intermediates. Specifically, an optically active 1-substituted amino-2,3-propanediol (1) is reacted with an orthoacid ester (2) or thionyl chloride (3) to produce a cyclic optically active compound (4), and then a compound (5) containing a halogen atom is prepared by reaction with a ring-opening reaction agent having an ability to introduce a halogen atom X. Finally, an optical active 1-substituted amino-2,3-epoxypropane is prepared by ring-closure reaction in the presence of a base.
本发明提供了一种工业过程,能够有效地和有利地制备出光学活性的1-取代
氨基-2,3-环氧
丙烷,该中间体可用于从光学活性的1-取代
氨基-2,3-
丙二醇原料制备农药和医药产品。本发明还提供了有用的中间体。具体而言,将光学活性的1-取代
氨基-2,3-
丙二醇(1)与正酸酯(2)或
硫酰氯(3)反应,以产生环状的光学活性化合物(4),然后通过与具有引入卤素原子X能力的环开放反应试剂反应,制备含有卤素原子的化合物(5)。最后,在碱存在下进行环闭合反应,制备光学活性的1-取代
氨基-2,3-环氧
丙烷。