Journal
TETRAHEDRON LETTERS
Volume 104, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2022.154045
Keywords
Mukayiama reagent; 1,2-Disubstituted-1H-benzo[d]imidazoles; Metal-free synthesis; Cyclization
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This article presents a rapid, metal-free, and straightforward method for synthesizing a series of 1,2-disubstituted-1H-benzo[d]imidazoles.
Within the field of medicinal chemistry, 1,2-disubstituted benzimidazoles represent a privileged class of nitrogen-based heterocycles but, unlike 2-substitued derivatives, few synthetic methods have been reported. In this context, we developed a rapid, metal-free, and straightforward method to prepare a series of 1,2-disubstituted-1H-benzo[d]imidazoles starting from 1,2-phenylendiamines and various aromatic and aliphatic aldehydes in the presence of the Mukaiyama reagent. The reaction proceeded at room temperature with good product yields within few minutes. (C) 2022 Elsevier Ltd. All rights reserved.
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