Practical Convergent Laboratory-Scale Synthesis Of A Ccr5 Receptor Antagonist

Jason B. Crawford,Gang Chen,Bryon Carpenter,Trevor Wilson, Jenny Ji,Renato T. Skerlj,Gary J. Bridger

Organic Process Research & Development（2012）

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摘要

An efficient laboratory-scale synthesis has been developed for the selective CCR5 antagonist 1. The convergent route has a longest linear sequence of nine steps (Is steps overall), and has overall yields of 18-25%. The route has enabled the preparation of 550 g of 1.

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Solid-Phase Synthesis

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