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在连续流动微反应器中由Lipozyme® TL IM催化的含糖类嘧啶衍生物的两步串联合成。

Two-step tandem synthesis of sugar-containing pyrimidine derivatives catalyzed by Lipozyme® TL IM in continuous-flow microreactors.

作者信息

Xie Han-Jia, Shao Wen-Xuan, Du Li-Hua, Zhang Ao-Ying, Lin Hang, Huang Zong-Hao, Fu Guo-Neng, Shen Jia-Hong, Yan Bing-Lin, Xue Miao-Miao, Wang Lin, Luo Xi-Ping

机构信息

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

Zhejiang Hisun Pharmaceutical Co., Ltd. Taizhou 318000 Zhejiang China

出版信息

RSC Adv. 2024 Dec 2;14(51):38193-38199. doi: 10.1039/d4ra07120d. eCollection 2024 Nov 25.

DOI:10.1039/d4ra07120d
PMID:39624429
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11610444/
Abstract

A novel series of sugar-containing pyrimidine derivatives have been synthesized an effective and convenient two-step tandem synthesis in continuous-flow microreactors with excellent regioselectivity. Using continuous-flow microreactors to assemble two-step reactions into one unit can effectively avoid separating and purifying intermediates. Moreover, this method allows the optimization of reaction parameters for each unit individually. The salient features of this method include a reduction in the use of DMSO and mild reaction conditions (30-40 °C). Under the optimum reaction conditions, we can obtain the desired yield (34.8-69.1%) in a shorter time (40 min) than the shaking condition (48 h).

摘要

通过连续流微反应器中的有效且便捷的两步串联合成，已合成了一系列新型的含糖嘧啶衍生物，具有出色的区域选择性。使用连续流微反应器将两步反应整合为一个单元，可有效避免中间体的分离和纯化。此外，该方法允许分别对每个单元的反应参数进行优化。此方法的显著特点包括减少二甲基亚砜的使用以及温和的反应条件（30 - 40°C）。在最佳反应条件下，我们能够在比振荡条件（48小时）更短的时间（40分钟）内获得所需产率（34.8 - 69.1%）。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/7c29e8e467dd/d4ra07120d-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/01bf786b9bfc/d4ra07120d-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/43c8133d0085/d4ra07120d-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/7515907140b1/d4ra07120d-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/34b8aa0a731e/d4ra07120d-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/d42be038764e/d4ra07120d-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/7c29e8e467dd/d4ra07120d-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/01bf786b9bfc/d4ra07120d-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/43c8133d0085/d4ra07120d-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/7515907140b1/d4ra07120d-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/34b8aa0a731e/d4ra07120d-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/d42be038764e/d4ra07120d-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7a2/11610444/7c29e8e467dd/d4ra07120d-f6.jpg

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