台州学院王磊团队报道了无溶剂条件下可切换多组分环化反应获得氟烷基化二氢嘧啶和嘧啶。相关研究成果发表在2024年2月23日出版的《中国化学》。

开发可切换的无溶剂多组分反应以构建高附加值产品是有机合成的重要需求。

该文中，研究人员详细介绍了通过无溶剂/添加剂[3+2+1]环化，从容易获得的烯胺、三氟乙醛水合物或1-乙氧基-2,2-二氟乙醇和脒盐酸盐开始，构建不同的4-氟烷基-1,4-二氢嘧啶和4-氟烷基-嘧啶的可切换策略的成功实施。该反应符合绿色合成的概念，并为获得有价值的氟化杂环提供了新的途径。

附：英文原文

Title: Switchable Multicomponent Cyclization Reactions to Access Fluoroalkylated Dihydropyrimidines and Pyrimidines under Solvent-Free Conditions

Author: Wanqing Zuo, Zhizhen Zhu, Yu Cheng, Lingling Zuo, Xiao Geng, Zhifang Li, Lei Wang

Issue&Volume: 2024-02-23

Abstract: The development of switchable solvent-free multicomponent reactions to build high-value-added products is an important demand for organic synthesis. Herein, we detailed the successful implementation of a switchable strategy for the construction of diverse 4-fluoroalkyl-1,4-dihydropyrimidines and 4-fluoroalkyl-pyrimidines via a solvent/additive-free [3 + 2 + 1] annulation, starting from readily available enamines, trifluoroacetaldehyde hydrate or 1-ethoxy-2,2-difluoroethanol and amidines hydrochloride. This reaction conforms to the concept of green synthesis, and provides a new avenue to access valuable fluorinated heterocycles.

DOI: 10.1002/cjoc.202300725

Source: https://onlinelibrary.wiley.com/doi/full/10.1002/cjoc.202300725