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Open AccessReview

Synthesis of Imidazole-Based Medicinal Molecules Utilizing the van Leusen Imidazole Synthesis

by Xunan Zheng 1,2, Zhengning Ma 1,3 and Dawei Zhang 1,*
College of Chemistry, Jilin University, Changchun 130012, China
College of Plant Science, Jilin University, Changchun 130062, China
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Ministry of Education), School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China
Author to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(3), 37;
Received: 10 February 2020 / Revised: 27 February 2020 / Accepted: 1 March 2020 / Published: 3 March 2020
(This article belongs to the Section Medicinal Chemistry)
Imidazole and its derivatives are one of the most vital and universal heterocycles in medicinal chemistry. Owing to their special structural features, these compounds exhibit a widespread spectrum of significant pharmacological or biological activities, and are widely researched and applied by pharmaceutical companies for drug discovery. The van Leusen reaction based on tosylmethylisocyanides (TosMICs) is one of the most appropriate strategies to synthetize imidazole-based medicinal molecules, which has been increasingly developed on account of its advantages. In this review, we summarize the recent developments of the chemical synthesis and bioactivity of imidazole-containing medicinal small molecules, utilizing the van Leusen imidazole synthesis from 1977. View Full-Text
Keywords: van Leusen; TosMICs; imidazole; synthesis van Leusen; TosMICs; imidazole; synthesis
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Zheng, X.; Ma, Z.; Zhang, D. Synthesis of Imidazole-Based Medicinal Molecules Utilizing the van Leusen Imidazole Synthesis. Pharmaceuticals 2020, 13, 37.

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