One-step synthesis of heteroaromatic-fused pyrrolidines via cyclopropane ring-opening reaction:: Application to the PKCβ inhibitor JTT-010

A ring-opening reaction of cyclopropanes with five-membered heteroaromatics having a leaving group at C(2) was found to provide heteroaromatic-fused pyrrolidines in one step. This reaction was successfully applied to the synthesis of the protein kinase C-beta inhibitor JTT-010, which possesses a dihydropyrrolo[1,2-a]indole core.