A morpholine-free process amenable convergent synthesis of apixaban: a potent factor Xa inhibitor

被引：6

作者：

Nevuluri, Narasimha Rao ^{[1
]}

Rapolu, Rajesh Kumar ^{[1
]}

Iqbal, Javed ^{[1
]}

Kandagatla, Bhaskar ^{[1
]}

Sen, Saikat ^{[1
]}

Dahanukar, Vilas H. ^{[2
]}

Oruganti, Srinivas ^{[1
]}

机构：

[1] Univ Hyderabad Campus, Dr Reddys Inst Life Sci, Ctr Proc Res & Innovat, Hyderabad 500046, Telangana, India

[2] Dr Reddys Labs, Integrated Prod Dev Org, Hyderabad 500090, Telangana, India

来源：

MONATSHEFTE FUR CHEMIE | 2017年 / 148卷 / 08期

关键词：

Anti-coagulant drug; Copper catalyzed N-arylation; Eliminations; Halogenation; Heterocycles; Pyrazole ring formation; VENOUS THROMBOEMBOLISM; BMS-562247;

D O I：

10.1007/s00706-017-1920-1

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A convergent synthesis of the anti-coagulant drug apixaban has been efficiently demonstrated on a multi-gram scale. The synthetic route is noteworthy for its brevity and fact that it completely avoids the use of morpholine, a toxic and flammable reagent, in constructing the 5,6-dihydro-1H-pyrazolo[ 3,4-c] pyridin-7(4H)-one core present in apixaban.

引用

页码：1477 / 1482

页数：6

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