Synthesis

… mediated, high-throughput, solution-phase synthesis of benzimidazoles from 1, 2-phenylenediamines and aldehydes and its application to preparative scale synthesis

PL Beaulieu, B Haché, E von Moos

Index: Beaulieu, Pierre L.; Hache, Bruno; Von Moos, Elisabeth Synthesis, 2003 , # 11 p. 1683 - 1692

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Citation Number: 162

Abstract

Abstract Addition of oxone® to a mixture of a 1, 2-phenylenediamine and an aldehyde in wet DMF at room temperature results in rapid formation of benzimidazoles under very mild conditions. The reaction is applicable to a wide range of substrates including aliphatic, aromatic and heteroaromatic aldehydes, and is not significantly affected by steric or electronic effects. In most cases, crude products are isolated in good to excellent yields ( ...