Campeau L.-C.,Global Process Chemistry |
Dolman S.J.,Global Process Chemistry |
Gauvreau D.,Global Process Chemistry |
Corley E.,Global Process Chemistry |
And 6 more authors.
Organic Process Research and Development | Year: 2011
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. © 2011 American Chemical Society.