An efficient multikilogram synthesis of ABT-963: A selective COX-2 inhibitor

被引：31

作者：

Kerdesky, FAJ ^{[1
]}

Leanna, MR ^{[1
]}

Zhang, J ^{[1
]}

Li, WK ^{[1
]}

Lallaman, JE ^{[1
]}

Ji, JG ^{[1
]}

Morton, HE ^{[1
]}

机构：

[1] Abbott Labs, Dept R450, Global Pharmaceut Res & Dev, N Chicago, IL 60064 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2006年 / 10卷 / 03期

关键词：

D O I：

10.1021/op060016v

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

An efficient chemical process for the multikilogram synthesis of ABT-963 ( 3) is described. The potent and selective COX-2 inhibitor was prepared in four steps in 36% overall isolated yield from commercially available 3,4-difluoroaniline ( 4). The chemistry, which required no chromatography, involved a facile one-pot synthesis of the pyridazinone core, a selective alkoxylation, a high yielding Suzuki coupling, and a very efficient oxidation.

引用

页码：512 / 517

页数：6

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