Process Research and Scale-up of a Commercialisable Route to Maraviroc (UK-427,857), a CCR-5 Receptor Antagonist

被引：32

作者：

Ahman, Jens ^{[1
]}

Birch, Melissa ^{[1
]}

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

Long, James ^{[1
]}

Wilder, Alexander ^{[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/op800062d

中图分类号：

O69 [应用化学];

学科分类号：

081704 [应用化学];

摘要：

A six-step synthetic route to the CCR-5 receptor antagonist Maraviroc (UK-427,857) (1) has been developed and demonstrated at scale in a pilot plant. The route has supported four Pilot-Plant campaigns and has produced multikilogram quantities of 1. Continued development of the synthetic route has resulted in a robust process with improved throughput compared to that of the original synthesis (Haycock-Lewandowski, S. J.; Mawby, N. J.; Wilder, A.; Ahman, J. Org. Process Res. Dev. 2008, 12, 1094-1103).

引用

页码：1104 / 1113

页数：10

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