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

被引：27

作者：

Jiang, Jian'an ^{[1
]}

Ji, Yafei ^{[1
]}

机构：

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

来源：

SYNTHETIC COMMUNICATIONS | 2013年 / 43卷 / 01期

关键词：

Apixaban; cost-effective synthetic route; inhibitor of blood coagulation factor Xa; 4-nitroaniline; THROMBOSIS;

D O I：

10.1080/00397911.2011.591956

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

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%).

引用

页码：72 / 79

页数：8

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