Rhodium‐Catalyzed Direct Arylation of Furopyridine: Synthesis and the Cardiac Effects of Dictamnine Derivatives

Abstract Herein is reported a Rh 2 (OAc) 4 /IMes ⋅ HCl system that promotes the chemoselective installation of aryl groups at the 2‐position of furo[2,3‐ b ]pyridine (53–94% yields). The method is applicable to the direct modification of the natural furoquinoline alkaloid dictamnine. The cardiac effects of the fluorinated analogues improved, compared to dictamnine at 160 μg/mL. Preliminary mechanism of action studies indicate that the effects might be related to epinephrine α receptors, M‐receptor, and calcium channel receptor. magnified image