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Published on: January 19, 2016
N-Formylation of Secondary Amines and Their Application in the Synthesis of Benzimidazole Derivatives Using DMF as a
Tomoya Sakaguchi1, Ryoma Nishio1, Hibiki Awata1
1Department of Applied Chemistry, Faculty of Engineering, Osaka Institute of Technology, 5-16-1 Ohmiya, Asahi, Osaka 535-8585, Japan.
Abstract:
Numerous methodologies for the N-formylation of amines using DMF as a formylating agent often require harsh conditions. Meanwhile, the synthesis of benzimidazole derivatives using DMF as a C1 source remains underexplored, with most methods relying on high temperatures and metal catalysts. In this study, we present a highly efficient N-formylation of amines at room temperature within 5 min utilizing the Vilsmeier reagent. Furthermore, we demonstrate its applicability in the synthesis of benzimidazole derivatives under milder conditions employing DMF as the C1 source.
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