Base-Promoted Formylation and N-Difluoromethylation of Azaindoles with Ethyl Bromodifluoroacetate as a Carbon Source

作     者：Yang Li Ning Sun Cai-Lin Zhang Meng Hao Yang Li;Ning Sun;Cai-Lin Zhang;Meng Hao

作者机构：Xi'an Key Laboratory of Textile Chemical Engineering AuxiliariesSchool of Environmental and Chemical EngineeringXi'an Polytechnic UniversityXi'anShaanxi 710048China 

出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)

年 卷 期：2021年第39卷第6期

页      面：1477-1482页

核心收录：

学科分类：07[理学] 070303[理学-有机化学] 0703[理学-化学] 

基　　金：the financial support from the National Natural Science Foundation of China(No.21503161) the Key Research&Development Project in Shaanxi Province(No.2017ZDXM-GY-040) the Doctoral Scientific Research Foundation of Xi'an Polytechnic University(No.107020336). 

主　　题：Azaindoles C1 building blocks Difluoromethylene Hydrolysis Synthetic methods 

摘      要：We reported for the first time that ethyl bromodifluoroacetate directly reacts with azaindole without transition metal catalysis to produce a difluoromethyl protected 5-aldehyde group product in one step.It is worth mentioning that the reacted aldehyde group is only formed at the 5 position.In addition,this method has good substrate applicability and functional group tolerance.Finally,we also carried out some mechanism auxiliary experiments,which confirmed that the aldehyde-based carbon comes from ethyl bromodifluoroacetate.