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

Xunan Zheng; Zhengning Ma; Dawei Zhang

doi:10.3390/ph13030037

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

Pharmaceuticals (Basel). 2020 Mar 3;13(3):37. doi: 10.3390/ph13030037.

Authors

Xunan Zheng^{1

2}, Zhengning Ma^{1

3}, Dawei Zhang¹

Affiliations

¹ College of Chemistry, Jilin University, Changchun 130012, China.
² College of Plant Science, Jilin University, Changchun 130062, China.
³ Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Ministry of Education), School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.

Abstract

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.

Keywords: TosMICs; imidazole; synthesis; van Leusen.

Publication types

Review