(R)-2-phenyl-4-(phenylmethyl)-1-(2-propenyl)hexahydropyrazine dihydrochloride 、 甲烷 、 sodium hydroxide 、 甲苯 在
三氯化钌甲苯 、 水 作用下,
以
水 为溶剂,
反应 24.0h,
以to obtain 227 mg of the title compound as pale brown oil (yield: 91%, chemical purity: 94.8 area %)的产率得到(R)-1-苄基-3-苯基哌嗪
参考文献:
名称:
METHOD FOR PRODUCING OPTICALLY ACTIVE 2-ARYLPIPERAZINE DERIVATIVE
Novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, enantiomers thereof or prodrugs thereof of Formula (I)
wherein the substituents are as defined herein, which are useful as therapeutic agents.
Method for producing optically active 2-arylpiperazine derivative
申请人:Kaneka Corporation
公开号:US08273883B2
公开(公告)日:2012-09-25
The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.