Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129

被引：18

作者：

Mitsuya, M ^{[1
]}

Kawakami, K ^{[1
]}

Ogino, Y ^{[1
]}

Miura, K ^{[1
]}

Mase, T ^{[1
]}

机构：

[1] Banyu Tsukuba Res Inst Merck Res Labs, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(99)00327-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A diastereoselective synthesis of J-104129 (1) was developed. A key step of this synthesis was Michael addition of enolate generated from cis-chiral dioxolane 2 to cyclopentenone, followed by hydrogenolysis of the resultant enol triflate 4. A mixture of cyclopentyldioxolane (5, 6) was hydrolyzed with sodium hydroxide to yield carboxylic acid 7 in 86% ee. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2037 / 2038

页数：2

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