Development of a green, concise synthesis of nicotinamide derivatives catalysed by Novozym® 435 from Candida antarctica in sustainable continuous-flow microreactors

An increasing number of studies have shown that many nicotinamide derivatives exhibited extensive biological activities, such as anti-inflammatory and antitumor activity. In this paper, a green, concise synthesis of nicotinamide derivatives in sustainable continuous-flow microreactors catalysed by N...

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Bibliographic Details
Published in:RSC Advances
Main Authors: Sheng, Zhi-Kai, Liu, Yi, Du, Li-Hua, Zhang, Shi-Yi, Zhang, Ao-Ying, Xie, Han-Jia, Lin, Hang, Yan, Bing-Lin, Xue, Miao-Miao, Ruan, Zhi-Xuan, Fu, Guo-Neng, Pan, Bing-Le, Zhou, Tong-Yao, Luo, Xi-Ping
Format: Text
Language:English
Published: The Royal Society of Chemistry 2024
Subjects:
Chemistry
Antarc*
Antarctica
Online Access:http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10758761/
http://www.ncbi.nlm.nih.gov/pubmed/38173597
https://doi.org/10.1039/d3ra07201k
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Summary:An increasing number of studies have shown that many nicotinamide derivatives exhibited extensive biological activities, such as anti-inflammatory and antitumor activity. In this paper, a green, concise synthesis of nicotinamide derivatives in sustainable continuous-flow microreactors catalysed by Novozym® 435 from Candida antarctica has been developed. Application of an easily obtainable and reusable lipase in the synthesis of nicotinamide derivatives from methyl nicotinate and amines/benzylamines reacted for 35 min at 50 °C led to high product yields (81.6–88.5%). Environmentally friendly tert-amyl alcohol was applied as a reaction medium. Substantially shorter reaction times as well as a significant increase in the product yield were obtained as compared to the batch process. This innovative approach provides a promising green, efficient and rapid synthesis strategy for pharmaceutical synthesis and further activity research of novel nicotinamide derivatives.

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