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For synthesis of intermediate and its preparation and use paroxetine 发明申请

2023-08-29 2430 764K 0

专利信息

申请日期 2025-06-25 申请号 JP2017513185
公开(公告)号 JP2017529343A 公开(公告)日 2017-10-05
公开国别 JP 申请人省市代码 全国
申请人 ZHEJIANG JIUZHOU PHARMACEUTICAL CO LTD
简介 A paroxetine intermediate, a method for preparing the same, and uses thereof are provided. Specifically, the method includes : reacting a compound of formula I below with a compound of formula II in the presence of an organic base under the catalysis of a complex formed from a chiral amine oxide L and a rare-earth metal compound Ln(OTf) 3 to prepare a compound of formula III below : wherein R 1 is alkyl, phenyl or benzyl; R 2 , R 3 , R 4 are each independently C 1 -C 6 alkyl or C 6 -C 10 aryl; the chiral amine oxide L has the following structure : wherein n = 1, 2; and R = Ph-, 2, 6-Me 2 C 6 H 3 -, 2, 6-Et 2 C 6 H 3 -, 2, 6-iPr 2 C 6 H 3 -, Ph 2 CH-.


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