Convergent kilo-scale synthesis of a potent renin inhibitor for the treatment of hypertension

…, D Steinhuebel, M Weisel, PD O'Shea

Index: Campeau, Louis-Charles; Dolman, Sarah J.; Gauvreau, Danny; Ouellet, Stephane G.; O'Shea, Paul D.; Corley, Ed; Liu, Jinchu; Guidry, Erin N.; Steinhuebel, Dietrich; Weisel, Mark Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1138 - 1148

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Citation Number: 12

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- ...