二氟卡宾促进的三氟甲基化和环化反应用于合成3-(三氟甲基)-4-吡喃。
Difluorocarbene-Enabled Trifluoromethylation and Cyclization for the Synthesis of 3-(Trifluoromethyl)-4-pyrans.
作者信息
Wu Chun-Yan, Chen Xiang-Long, Yang Dong-Sheng, Tang Yong-Xing, Wang Li-Sheng, Du Yong-Dong, Wu Yan-Dong, Wu An-Xin
机构信息
State Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan, Hubei 430079, China.
State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China.
出版信息
Org Lett. 2024 Oct 11;26(40):8589-8593. doi: 10.1021/acs.orglett.4c03266. Epub 2024 Sep 27.
A three-component annulation reaction and trifluoromethylation for the construction of 3-(trifluoromethyl)-4-pyrans using β-CF-1,3-enynes, BrCFCOEt, and sulfoxonium ylides as readily available substrates has been developed. This metal-free process involves two C-F bond cleavages of β-CF-1,3-enynes and a CF group generated from BrCFCOEt. This method is applicable to the late-stage modification of pharmaceutically active molecules.
已开发出一种三组分环化反应和三氟甲基化反应，用于使用β-CF-1,3-烯炔、BrCFCOEt和亚砜叶立德作为易得底物构建3-(三氟甲基)-4-吡喃。这种无金属过程涉及β-CF-1,3-烯炔的两次C-F键裂解以及由BrCFCOEt生成的CF基团。该方法适用于药物活性分子的后期修饰。
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