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- Title
Microfluidics Biocatalysis System Applied for the Synthesis of N-Substituted Benzimidazole Derivatives by Aza-Michael Addition.
- Authors
Jiang, Rong-Kuan; Pan, Yue; Du, Li-Hua; Zheng, Ling-Yan; Sheng, Zhi-Kai; Zhang, Shi-Yi; Lin, Hang; Zhang, Ao-Ying; Xie, Han-Jia; Yang, Zhi-Kai; Luo, Xi-Ping
- Abstract
Benzimidazole scaffolds became an attractive subject due to their broad spectrum of pharmacological activities. In this work, a methodology was developed for the synthesis of N-substituted benzimidazole derivatives from benzimidazoles and α, β-unsaturated compounds (acrylonitriles, acrylate esters, phenyl vinyl sulfone) catalyzed by lipase TL IM from Thermomyces lanuginosus in continuous-flow microreactors. Investigations were conducted on reaction parameters such as solvent, substrate ratio, reaction temperature, reactant donor/acceptor structures, and reaction time. The transformation is promoted by inexpensive and readily available lipase in methanol at 45 °C for 35 min. A wide range of β-amino sulfone, β-amino nitrile, and β-amino carbonyl compounds were efficiently and selectively synthesized in high yields (76–97%). All in all, a microfluidic biocatalysis system was applied to the synthesis of N-substituted benzimidazole derivatives, and could serve as a promising fast synthesis strategy for further research to develop novel and highly potent active drugs.
- Subjects
BENZIMIDAZOLE derivatives; BIOCATALYSIS; MICROFLUIDICS; ACRYLONITRILE; CARBONYL compounds; BENZIMIDAZOLES; SULFONES
- Publication
Catalysts (2073-4344), 2022, Vol 12, Issue 12, p1658
- ISSN
2073-4344
- Publication type
Article
- DOI
10.3390/catal12121658