Convergent Kilo-Scale Synthesis of a Potent Renin Inhibitor for the Treatment of Hypertension
Organic Process Research & Development2011Vol. 15(5), pp. 1138–1148
Citations Over TimeTop 12% of 2011 papers
Louis‐Charles Campeau, Sarah J. Dolman, Danny Gauvreau, Ed Corley, Li Li, Erin N. Guidry, Stéphane G. Ouellet, Dietrich Steinhuebel, Mark Weisel, Paul O’Shea
Abstract
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.
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