Combinatorial Synthesis of Substituted Pyrazolo-Fused Quinazolines by the Rh(III)-Catalyzed [5+1] Annulation of Phenyl-1H-pyrazol-5-amine with Alkynoates and Alkynamide

A Rh( iii )-catalyzed C–H activation/cyclization cascade is developed for the first divergent synthesis of pyrazolo[1,5- a ]quinazolines through a [5 + 1] annulation reaction exclusively.