Kilogram-Scale Synthesis of the CXCR4 Antagonist GSK812397

被引：78

作者：

Boggs, Sharon ^{[2
]}

Elitzin, Vassil I. ^{[1
]}

Gudmundsson, Kristjan ^{[2
]}

Martin, Michael T. ^{[1
]}

Sharp, Matthew J. ^{[1
]}

机构：

[1] GlaxoSmithKline Inc, Chem Dev, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline Inc, Infect Dis Ctr Excellence Drug Discovery, Res Triangle Pk, NC 27709 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2009年 / 13卷 / 04期

关键词：

D O I：

10.1021/op9000675

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

An improved, scalable synthesis of the CXCR4 antagonist GSK812397 is described. This new route was recently scaled up in 50 L fixed equipment to afford 1.2 kg of drug substance in five steps with an overall yield of 20% and >99% chemical and enantiomeric purity.

引用

页码：781 / 785

页数：5

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