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

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• 作者：Jens Å ; hman ; Melissa Birch ; Sarah J. Haycock-Lewandowski ; James ; Long ; Alexander Wilder
• 刊名：Organic Process Research & Development
• 出版年：2008
• 出版时间：November 21, 2008
• 年：2008
• 卷：12
• 期：6
• 页码：1104-1113
• 全文大小：320K
• 年卷期：v.12,no.6(November 21, 2008)
• ISSN：1520-586X

文摘

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).