Expanding the Synthetic Horizons of Iqbal MCR to Heterocyclics: Bioisosteric α‐Acylaminopyrazoles as Ugi α‐ Acylamino Carboxamide Mimetics

This study reports a novel and efficient synthetic method for accessing di‐ and tri‐ substituted α‐acylaminopyrazole scaffolds, potential bioisosteric replacements for Ugi α‐acylamino carboxamide scaffolds. A diverse library of these α‐acylaminopyrazoles was generated via a Cu(II)‐catalyzed sequential Iqbal MCR/Knorr heterocyclization at room temperature. This two‐step protocol consistently yielded products in moderate‐to‐good yields and purity, eliminating the need for column chromatography. In silico ADME predictions further support their potential as bioisosteric replacements and suggest promising oral bioavailability.