Synthesis of the optical isomers of a new anticholinergic drug, penehyclidine hydrochloride (8018)

被引：85

作者：

Han, XY ^{[1
]}

Liu, H ^{[1
]}

Liu, CH ^{[1
]}

Wu, B ^{[1
]}

Chen, LF ^{[1
]}

Zhong, BH ^{[1
]}

Liu, KL ^{[1
]}

机构：

[1] Beijing Inst Pharmacol & Toxicol, Dept 7, Beijing 100850, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 08期

基金：

中国国家自然科学基金;

关键词：

asymmetric; epoxidation; isomers; penehyclidine; hydrochloride;

D O I：

10.1016/j.bmcl.2005.02.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A practical diastereoselective synthetic method for 8018 enantiopure isomers is described. The intramolecular asymmetric epoxidation of mono-sulfonate 4 was applied for the execution of the synthesis of the key chiral building block for the first time. The isomers were obtained with 70-76% yields in 99-100% ee. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1979 / 1982

页数：4

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