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

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posted on 2025-12-03, 17:19 authored by Safomuddin Abduahadi, Emmanuel Mintah Bonku, Jun Lin, Sodik Numonov, Farukh Sharopov, Fuqiang Zhu, Samuel Desta Guma, Hongjian Qin, Jingshan Shen
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.

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