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
• 来源期刊: 中国化学（英文版）
• 年，卷（期）: 2021,（6）
• 所属期刊栏目: Concise Reports
• 页码范围: 1477-1482
• 页数: 6页
• 语种: 英文
• DOI: 10.1002/cjoc.202100008

摘要

Main observation and conclusion 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 al-so carried out some mechanism auxiliary experiments,which confirmed that the aldehyde-based carbon comes from ethyl bromo-difluoroacetate.