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A short synthesis of the parp inhibitor 2-(4-trifluoro-methylphenyl)benzimidazole-4-carboxamide (NU1077)

✍ Scribed by Steven C. Austen; John M. Kane

Publisher: Journal of Heterocyclic Chemistry
Year: 2001
Tongue: English
Weight: 26 KB
Volume: 38
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.5570380427

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✦ Synopsis

Abstract

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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