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

Authors
Austen, SC Kane, JM
Citation
Sc. Austen et Jm. Kane, A short synthesis of the PARP inhibitor 2-(4-trifluoromethylphenyl)benzimidazole-4-carboxamide (NU1077), J HETERO CH, 38(4), 2001, pp. 979-980
Citations number
18
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
JOURNAL OF HETEROCYCLIC CHEMISTRY
ISSN journal
0022152X → ACNP
Volume
38
Issue
4
Year of publication
2001
Pages
979 - 980
Database
ISI
SICI code
0022-152X(200107/08)38:4<979:ASSOTP>2.0.ZU;2-S
Abstract
A four-step synthesis of the PARP inhibitor 2-(4-trifluoromethylphenyl)benz imidazole-4-carboxamide (1, NU1077) is presented. Condensation of 2,3-diami notoluene and 4-trifluoromethylbenzaldehyde afforded 4-methyl-2-(4-trifluor omethylphenyl)benzimidazole. Oxidation of the methyl group with potassium p ermanganate in warm t-butanol afforded the carboxylic acid that was convert ed to the corresponding carboxamide via the acid chloride.