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在可持续连续流动微反应器中，由诺维信435催化的烟酰胺衍生物绿色简洁合成方法的开发。

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

作者信息

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

机构信息

College of Pharmaceutical Science, ZheJiang University of Technology Zhejiang Hangzhou 310014 China

Zhejiang Provincial Key Laboratory of Chemical Utilization of Forestry Biomass, Zhejiang A&F University Zhejiang Hangzhou 311300 China.

出版信息

RSC Adv. 2024 Jan 2;14(1):131-138. doi: 10.1039/d3ra07201k.

DOI:10.1039/d3ra07201k
PMID:38173597
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10758761/
Abstract

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 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 -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.

摘要

越来越多的研究表明，许多烟酰胺衍生物具有广泛的生物活性，如抗炎和抗肿瘤活性。本文开发了一种在可持续连续流微反应器中，由诺维信435催化的绿色、简洁合成烟酰胺衍生物的方法。使用一种易于获得且可重复使用的脂肪酶，催化烟酸甲酯与胺类/苄胺类反应35分钟，在50℃下合成烟酰胺衍生物，可获得较高的产物收率（81.6 - 88.5%）。采用环境友好的叔戊醇作为反应介质。与间歇法相比，反应时间显著缩短，产物收率显著提高。这种创新方法为新型烟酰胺衍生物的药物合成和进一步活性研究提供了一种有前景的绿色、高效、快速的合成策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/6432cf25398e/d3ra07201k-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/32f5819b106b/d3ra07201k-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/78d9ec54ff3e/d3ra07201k-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/4c7c0b9044a0/d3ra07201k-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/51702efab569/d3ra07201k-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/8dd212ddec2c/d3ra07201k-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/a710fd39dc09/d3ra07201k-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/6432cf25398e/d3ra07201k-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/32f5819b106b/d3ra07201k-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/78d9ec54ff3e/d3ra07201k-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/4c7c0b9044a0/d3ra07201k-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/51702efab569/d3ra07201k-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/8dd212ddec2c/d3ra07201k-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/a710fd39dc09/d3ra07201k-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ca1/10758761/6432cf25398e/d3ra07201k-f6.jpg

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