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Note | Special issue | Vol 70, No. 1, 2006, pp.571-580
Published online, 2nd November, 2006
DOI: 10.3987/COM-06-S(W)25
A Facile Synthesis of 2-Acyl and 2-Alkylaminobenzimidazoles for 5-Lipoxygenase Inhibitors

Jin Ha Lee, Mi Hyun Ahn, Eun Hyun Choi, Hea-Young Park Choo, and Gyoonhee Han*

*Department of Biotechnology, College of Engineering, 134 Shinchon-dong, Seodaemun-gu, Seoul 120-749, Korea


2-Acylaminobenzimidazoles (2a-r) have been synthesized from o-phenylenediamines (4) with benzoylcarbonimidodithioic acid dimethyl ester (5a) or dimethyl isobutyrylcarbonimidodithioic acid dimethyl ester (5b) in good yield. 2-Alkylaminobenzimidazoles could be prepared by the reaction of o-Phenylenediamines (4a, b) with benzyl isothiocyanate in moderate yields 8a, b or the reaction of 2-chlorobenzimidazole (9) with benzylamines (10a, b) in moderate yield 11a, b. Finally, the carbamate derivative of 2-aminobenzimidazole (13) was prepared by the reaction with pseudourea (12) in low yield. Most of the prepared analogues were evaluated in leukotriene inhibition assay and it found that benzamide derivatives (2a-i) are quite active among others.