A regioselective arylative cyclization of ortho functional diaryl acetylenes for the synthesis of selectively substituted diaryl pyridine and indene derivatives is accomplished through an electrophile driven alkyne polarization.
In the realm of transition-metal catalyzed arene functionalization, rhodium(III) catalysis is considered as exemplary due to its propensity to activate C−H bonds to obtain comprehensive molecular assembly. Herein, we demonstrate a new rhodium(III) catalyzed assembly of polyheterocyclic scaffolds via C−H activation and regioselective annulation of 4-arylbut-3-yn-1-amines with 4-hydroxy-2-alkynoates. Heterocyclization and transmetalation prior to annulation is the key for initiation of this relay redox-neutral catalytic cascade.
The efficiency and selectivity of annulation reactions are often difficult to control in the presence of multiple potential reactive centers, like in case of allylic sulfur ylides (ASY). Here, we...
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