Convergent Kilo-Scale Synthesis of a Potent Renin Inhibitor for the Treatment of Hypertension

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• 作者：Louis-Charles Campeau ; Sarah J. Dolman ; Danny Gauvreau ; Ed Corley ; Jinchu Liu ; Erin N. Guidry ; Ste虂phane G. Ouellet ; Dietrich Steinhuebel ; Mark Weisel ; Paul D. O鈥橲hea
• 刊名：Organic Process Research & Development
• 出版年：2011
• 出版时间：September 16, 2011
• 年：2011
• 卷：15
• 期：5
• 页码：1138-1148
• 全文大小：1046K
• 年卷期：v.15,no.5(September 16, 2011)
• ISSN：1520-586X

文摘

Process research and development of a synthetic route towards a novel renin inhibitor (1) is described. The highly convergent synthetic route provided 1 in 15% yield on multikilogram scale with a longest linear sequence of 11 steps. The use of catalytic hydrogenation features prominently in our design. The proper choice of N-methylpyridone surrogate was also important, and we describe a method for the easy conversion of 2-methoxypyridines to N-methylpyridones using cheap and readily available reagents.