Conversion of sterically hindered diacylated 1, 2-phenylenediamines into 2-substituted benzimidazoles

J Charton, S Girault-Mizzi, C Sergheraert

Index: Charton, Julie; Girault-Mizzi, Sophie; Sergheraert, Christian Chemical and Pharmaceutical Bulletin, 2005 , vol. 53, # 5 p. 492 - 497

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Citation Number: 29

Abstract

A series of bulky 2-substituted benzimidazoles was designed in order to find new leads for several biological targets. Formation by cyclodehydration from their monoacylated counterparts was shown to be strongly dependent upon the nature of the acyl group. In the case of a dicyclohexylmethyl group, cyclization was only observed in a p-toluenesulfonic acid/toluene mixture from the symmetrical diacylated precursor. Analysis of the ...