作者: Sylvestre P. J. T. Bachollet , Jérôme F. Vivat , Dean C. Cocker , Harry Adams , Joseph P. A. Harrity
关键词:
摘要: The aza-Diels–Alder cycloaddition of 1,2,4-triazines with alkynes offers a rapid and convenient method for the synthesis highly substituted pyridines, but often requires harsh conditions long reaction times. present study solution to these limitations by use temporary tether established Lewis acid–base complexation in situ generated alkynylboranes triazines bearing basic donor. reactions take place within 20 min at 40 °C provide direct access broad range pyridines complete predictable regiocontrol. carbon[BOND]boron bond can be further functionalised cross-coupling allowing functionality introduced after cycloaddition.