Key result
A highly convergent synthetic route provided a novel renin inhibitor in 15% yield on a multikilogram scale over 11 steps.
May enable further preclinical and clinical evaluation of renin inhibition; leaves open therapeutic utility in cardiovascular disease.
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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Campeau et al. (2011) studied Hypertension. Renin inhibitor (1) was evaluated on Synthesis yield. A highly convergent synthetic route provided a novel renin inhibitor in 15% yield on a multikilogram scale over 11 steps.
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