Development of a Bulk Enabling Route to Maraviroc (UK-427,857), a CCR-5 Receptor Antagonist

被引：90

作者：

Haycock-Lewandowski, Sarah J. ^{[1
]}

Wilder, Alexander ^{[1
]}

Ahman, Jens ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Dept Chem Res & Dev, Sandwich CT13 9NJ, Kent, England

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2008年 / 12卷 / 06期

关键词：

D O I：

10.1021/op8000614

中图分类号：

O69 [应用化学];

学科分类号：

081704 [应用化学];

摘要：

A bulk enabling synthesis of the CCR-5 receptor antagonist, Maraviroc (UK-427,857) (1), is presented. Synthesis of the three key fragments, beta-amino ester 3, 4,4-difluorohexanecarboxylic acid (2), and 1,3,4-triazole-substituted tropane fragment 4 are described. Coupling strategies for these fragments are discussed and described, including synthetic challenges, protection strategies, impurity generation, and final scale-up of the developed route to 1.

引用

页码：1094 / 1103

页数：10

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