Abstract The synthesis of a designed, sterically congested geminal dimethyl-bearing PAR-1 antagonist was achieved by a route of ten steps, with the oxidation of an electron-rich benzaldehyde, the construction of a tertiary alkyl azide, and the selective hydrogenolysis of a 1, 5-fused tetrazole to generate the cyclic amidine with Raney-Ni being the key steps. The selective hydrogenolysis of 1, 5-fused tetrazole to generate the cyclic amidine with Raney- ...
