Iodine-Promoted Ring-Opening α,β-Difunctionalization of Cyclopropanols with Enaminones: A Selective Route to 2,4-Diacylpyrroles

In this work, we report a novel I2-mediated ring-opening α,β-difunctionalization of cyclopropyl alcohols with enaminones for the first time. The selective [3 + 2] annulation instead of [3 + 3] annulation under metal-free conditions enables a straightforward and efficient synthesis of structurally important 2,4-diacylpyrroles. Notably, this methodology dispenses with metal catalysts, proceeds under mild reaction conditions, and features not only simple operation but also suitability for gram-scale preparation and late-stage functionalization of complex bioactive molecules.