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1.发明专利Method for synthesizing (+) and (-)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane 有权合成（+）和（ - ） - 1-（3,4-二氯苯基）-3-亚甲基[[3.1.0] HEXANE的方法
公开(公告)号：JP2014040422A
公开(公告)日：2014-03-06
申请号：JP2013181165
申请日：2013-09-02
发明人： CORLEY EDWARD G , SIMMONS BRYON , FENG SUE , JERRY A MURRY
IPC分类号： C07D209/52 , C07C211/29 , C07C215/38 , C07C255/46
CPC分类号： C07C255/46 , C07C211/29 , C07C215/20 , C07C215/38 , C07C2601/02 , C07D209/52
摘要： PROBLEM TO BE SOLVED: To provide a simple and highly efficient method for producing (+) and (-)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexanes which are useful as active ingredients of therapeutic agents for depression, anxiety disorders, eating disorders, and urinary incontinence, or their pharmaceutically acceptable salts.SOLUTION: A method for producing (+) and (-)-l-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexanes or a pharmaceutically acceptable salt thereof includes: (1) a step of making 3,4-dichlorophenylacetonitrile and an optically active epichlorohydrin react with each other to obtain a cyclopropyl compound; (2) a step of reducing the cyclopropyl compound with a reducing agent to obtain an amino alcohol compound; (3) a step of chlorinating the amino alcohol compound with a chlorinating agent to obtain a chloro compound; and (4) a step of cyclodehydrating the chloro compound with a base.
摘要翻译： 要解决的问题：提供一种用于制备（+）和（ - ） - 1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷的简单且高效的方法，其可用作治疗剂的活性成分 抑制症，焦虑障碍，进食障碍和尿失禁药物或其药学上可接受的盐。方法：制备（+）和（ - ） - 1-（3,4-二氯苯基）-3-氮杂双环[3.1。 0]己烷或其药学上可接受的盐包括：（1）使3,4-二氯苯基乙腈和光学活性表氯醇彼此反应以获得环丙基化合物的步骤; （2）用还原剂还原环丙基化合物以获得氨基醇化合物的步骤; （3）用氯化剂氯化氨基醇化合物以获得氯化合物的步骤; 和（4）将氯化合物与碱进行环化脱水的步骤。
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