One-Pot Cyclocondensation Approach to Form 4-Amino-2-Pyridones via Ammonium Acetate as a Nitrogen Source
Safomuddin Abduahadi1,2, Emmanuel Mintah Bonku1, Jun Lin3
1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai 201203, P. R. China.
None:
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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