LiCl-promoted amination of beta-methoxy amides (gamma-lactones)

摘要

An efficient and mild method has been developed for the amination of beta-methoxy amides (gamma-lactones) including natural products michelolide, costunolide and parthenolide derivatives by using lithium chloride in good yields. This reaction is applicable to a wide range of substrates with good functional group tolerance. Mechanism studies show that the reactions undergo a LiCl promoted MeOH elimination from the substrates to form the corresponding alpha,beta-unsaturated intermediates followed by the Michael addition of amines.