Exquisite Synthesis of a Designed PAR??1 Antagonist

…, GL Zhao, LS Zhang, H Shao, JW Wang

Index: Miao, Hua-Ming; Zhao, Gui-Long; Zhang, Lin-Shan; Shao, Hua; Wang, Jian-Wu Helvetica Chimica Acta, 2011 , vol. 94, # 11 p. 1981 - 1993

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Citation Number: 3

Abstract

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- ...