Development of a Fit-for-Purpose Large-Scale Synthesis of an Oral PARP Inhibitor

被引：40

作者：

Wallace, Debra J. ^{[1
]}

Baxter, Carl A. ^{[1
]}

Brands, Karel J. M. ^{[1
]}

Bremeyer, Nadine ^{[1
]}

Brewer, Sarah E. ^{[1
]}

Desmond, Richard ^{[2
]}

Emerson, Khateeta M. ^{[1
]}

Foley, Jennifer ^{[2
]}

Fernandez, Paul ^{[3
]}

Hu, Weifeng ^{[4
]}

Keen, Stephen P. ^{[1
]}

Mullens, Peter ^{[1
]}

Muzzio, Daniel ^{[3
]}

Sajonz, Peter ^{[2
]}

Tan, Lushi ^{[2
]}

Wilson, Robert D. ^{[1
]}

Zhou, George ^{[3
]}

Zhou, Guoyue ^{[4
]}

机构：

[1] Global Proc Chem, Merck Sharp & Dohme Res Labs, Hoddesdon EN11 9BU, Herts, England

[2] Global Proc Chem, Merck Res Labs, Rahway, NJ 07065 USA

[3] Merck & Co Inc, Dept Chem Proc Dev & Commercializat, Rahway, NJ 07065 USA

[4] WuXi APPTec Shanghai Pharmaceut Co Ltd, Waigaoqiao Free Trade Zone, Shanghai 200131, Peoples R China

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2011年 / 15卷 / 04期

关键词：

HYDRAZOIC ACID; CYCLIZATION;

D O I：

10.1021/op2000783

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Compound (1) a poly(ADP-ribose)polymerase (PARP) inhibitor has been made by a fit-for-purpose large-scale synthesis using either a classical resolution or chiral chromatographic separation. The development and relative merits of each route are discussed, along with operational improvements and extensive safety evaluations of potentially hazardous reactions.

引用

页码：831 / 840

页数：10

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