Abstract

Direct, efficient syntheses of the benzimidazo[2,1- a]isoquinoline ring system have been achieved with 2-bromoarylaldehydes, terminal alkynes, and 1,2-phenylenediamines by a microwave-accelerated tandem process in which a Sonogashira coupling, 5- endo cyclization, oxidative aromatization, and 6- endo cyclization can be performed in a single synthetic operation.

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