Scalable Diboron-Catalyzed Amidation for the Synthesis of Amide-Based APIs

In this study, we explored the application of the tetrahydroxydiboron [B 2 (OH) 4 ] catalyst for the synthesis of amide-based active pharmaceutical ingredients (APIs), a key starting material (KSM), and amide derivatives of the drug, with water as the only byproduct. Notably, the protocol allows a simple acid–base workup for isolation of the pure amide derivatives, highlighting its practical and industrial relevance. Furthermore, the successful scale-up of challenging aromatic APIs from 1 to 10 g demonstrated the robustness and practical applicability of this methodology.