Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 12, Issue 6, Pages 1094-1103Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op8000614
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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.
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