Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Conversion of Sterically Hindered Diacylated 1,2-Phenylenediamines into 2-Substituted Benzimidazoles
Julie ChartonSophie Girault-MizziChristian Sergheraert
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2005 Volume 53 Issue 5 Pages 492-497

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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 mechanism was begun starting from mixed diacylated derivatives.
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© 2005 The Pharmaceutical Society of Japan
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