New Procedure for the Preparation of (1R,2R)-2-[(R)-3-(Benzyloxy)pyrrolidin-1-yl]cyclohexanol

被引：5
|
作者：
Ye, Haiwei [1 ]
Yu, Chuanming [1 ]
Zhong, Weihui [1 ]
机构：
[1] Zhejiang Univ Technol, Coll Pharmaceut Sci, Minist Educ, Key Lab Pharmaceut Engn, Hangzhou 310014, Zhejiang, Peoples R China
来源：
SYNTHESIS-STUTTGART | 2012年 / 44卷 / 01期
基金：
中国国家自然科学基金;
关键词：
(1R; 2R)-2-[(R)-3-(benzyloxy)pyrrolidin-1-yl]cyclohexanol; vernakalant; enantioselectivity; VERNAKALANT HYDROCHLORIDE; ATRIAL-FIBRILLATION; CONTROLLED-TRIAL; RSD1235;
D O I：
10.1055/s-0031-1289619
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A novel route to an intermediate of vernakalant, (1R,2R)-2-[(R)-3-(benzyloxy)pyrrolidin-1-yl]cyclohexanol from ethyl (R)-4-chloro-3-hydroxybutanoate is described. It was found that the key intermediate (R)-4-(benzyloxy)-1-[(1R,2R)-2-(tert-butyldimethylsiloxy)cyclohexyl]pyrrolidin-2-one\ could be isolated with high diastereomeric excess (up to 99% de) from its isomer by column chromatography alone, without further chemical resolution.
引用
收藏
页码：51 / 56
页数：6
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