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α-Chymotrypsin-catalyzed synthesis of 2-substituted benzimidazole through retro-Claisen reaction

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journal contribution
posted on 2018-11-03, 19:57 authored by Lian-Sheng Liu, Zong-Bo Xie, Can Zhang, Lei-Han Fu, Hai-Bo Zhu, Zhang-Gao Le

Benzimidazoles are important components of pharmaceutical compounds owing to their promising bioactivities. The green, safe, and efficient synthesis of benzimidazoles has always been one of the hot topics for chemical workers. α-Chymotrypsin-catalyzed synthesis of benzimidazoles was developed by a reaction between β-keotester and o-phenylenediamine via retro-Claisen reaction. In this eco-friendly medium, a variety of benzimidazole derivatives were obtained in good to excellent yields, with just 10 mg/mL α-Chymotrypsin as catalyst.

Funding

This project was supported by the National Natural Science Foundation of China [grant numbers 21462001, 21262002, 21465002], the Science and Technology Projects of Jiangxi [grant number 20161BCB24006], and the Science and Technology Foundation of the Jiangxi Education Department [grant numbers KJLD14050, GJJ150584].

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