文献类型：期刊文献

英文题名：ALTERNATE SYNTHESIS OF APIXABAN (BMS-562247), AN INHIBITOR OF BLOOD COAGULATION FACTOR XA

作者：Jiang, Jian'an[1];Ji, Yafei[1]

机构：[1]E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

年份：2013

卷号：43

期号：1

起止页码：72

外文期刊名：SYNTHETIC COMMUNICATIONS

收录：;EI(收录号：20242616515038);WOS:【SCI-EXPANDED(收录号:WOS:000308466500009)，CCR-EXPANDED(收录号:WOS:000308466500009)】；

语种：英文

外文关键词：Apixaban; cost-effective synthetic route; inhibitor of blood coagulation factor Xa; 4-nitroaniline

摘要：An alternate approach to apixaban was described. The synthesis features a novel and cost-effective synthetic strategy to construct a key N-phenylvalerolactam intermediate 4 from 4-nitroaniline. In addition, the modified synthetic route avoids the use of expensive reagents and significantly improves reaction yields. As demonstrated practically, apixaban was successfully synthesized in overall good yield (35%).