One-Pot Cyclocondensation Approach to Form 4-Amino-2-Pyridones via Ammonium Acetate as a Nitrogen Source

Despite significant progress in 2-pyridone applications for drug discovery, synthesizing 4-amino-2-pyridones remains challenging due to the difficulty of incorporating two nitrogen atoms into this scaffold. Herein, we describe a versatile three-step, one-pot synthesis of a variety of 4-amino-2-pyridones via a cyclocondensation reaction using ammonium acetate as a nitrogen source for the simultaneous formation of two new C-N bonds. The process demonstrates excellent scalability, producing quantities up to 100 g in a lab.