Abstract

A mild, sequential multicomponent reaction strategy for the regioselective synthesis of functionalized pentasubstituted pyrroles from readily accessible primary amines, 1,2-diaza-1,3-dienes, and 2,3-allenoates, has been developed. The process allows a [1N+2C+2C] annulation to be achieved through two sequential hydroamination reactions followed by an enamine-carbocyclization. Moreover, allenoates, as synthetic equivalents of monoactived alkynes, permit the specific preparation of multifunctionalized pyrroles.

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