An improvement to the preparation of prasugrel hydrochloride

作者:Ou Wenhua*; Yi Weiyin; Liu Feng; Pan Xianhua; Peng Xijiang
来源:Journal of Chemical Research, 2013, 37(6): 369-371.
DOI:10.3184/174751913X13687269227225

摘要

An efficient synthesis of prasugrel, a thienopyridine ADP-receptor antagonists, is described. A thienopyridine intermediate was prepared by N-protection, boric acid substitution and N-substitution. After acid hydrolysis of the methyl ether and subsequent acetylation, prasugrel was obtained with a total yield of 50% after seven linear steps from 4,5,6,7-tetrahydrothieno [3,2-c] pyridine and 2-bromo-1-cyclopropyl-2-(2-fluorophenyl) ethan-1-one as raw materials.