Development of a Multikilogram Scale Synthesis of a TRPV1 Antagonist

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• 作者：Jeffrey T. Kuethe ; Michel Journet ; Zhihui Peng ; Dalian Zhao ; Arlene McKeown ; Guy R. Humphrey
• 刊名：Organic Process Research & Development
• 出版年：2016
• 出版时间：February 19, 2016
• 年：2016
• 卷：20
• 期：2
• 页码：227-232
• 全文大小：294K
• ISSN：1520-586X

文摘

A highly efficient, regioselective five-step synthesis of the TRPV1 antagonist 1 is described. The coupling of piperazine 7 with dichloropyrimidine 8 proceeded via a regioselective Pd-mediated amination affording product 11 in excellent yield. Conversion of the penultimate product 14 afforded 1 through formation of a magnesium ate complex and trapping with CO₂.