ALKYLATION OF AZOLES

摘要

In one aspect, methods for the alkylation of azoles are described herein. In some embodiments, a method for the C2 alkylation of an azole compound comprises providmg an azolium salt comprising an N-allyl substituent, reacting the N-allyl azolium salt with an aldehyde to provide a reaction product mixture comprising a ketone and N-allyl-N,X- ketene acetal, and providing the C2-alkylated azole compound by Claisen rearrangement of the N-allyl-N,X-ketene acetal, wherein X is selected from the group consisting of S, N and O.