posted on 2025-12-03, 17:19authored bySafomuddin 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.