A short synthesis of the PARP inhibitor 2-(4-trifluoromethylphenyl)benzimidazole-4-carboxamide (NU1077)

被引：48

作者：

Austen, SC ^{[1
]}

Kane, JM ^{[1
]}

机构：

[1] Aventis Pharmaceut Inc, Cincinnati, OH 45215 USA

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2001年 / 38卷 / 04期

关键词：

D O I：

10.1002/jhet.5570380427

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A four-step synthesis of the PARP inhibitor 2-(4-trifluoromethylphenyl)benzimidazole-4-carboxamide (1, NU1077) is presented. Condensation of 2,3-diaminotoluene and 4-trifluoromethylbenzaldehyde afforded 4-methyl-2-(4-trifluoromethylphenyl)benzimidazole. Oxidation of the methyl group with potassium permanganate in warm t-butanol afforded the carboxylic acid that was converted to the corresponding carboxamide via the acid chloride.

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页码：979 / 980

页数：2

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