The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS, 2aR,14aR)-cyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2-[[7-methoxy-8-methyl-2-[4-10 (1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.
本发明涉及一种改进的制备过程,用于制备(2R,3aR,10Z,11aS,2aR,14aR)-环戊[c]环丙[a][1,6]二氮杂环十四烯-12a(1H)-
羧酸,2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-十四氢-2-[[7-甲氧基-8-甲基-2-[4-10(1-甲基乙基)-2-
噻唑基]-4-
喹啉基]氧基]-5-甲基-4,14-二氧基-,
乙酯。该化合物是大环化合物TMC 435的总合成路线中的中间体。TMC 435是
NS3/4A
蛋白酶的
抑制剂,对丙型肝炎病毒的复制起重要作用。