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.
Authors
- Jingshan Shen (ORCID: https://orcid.org/0000-0001-9679-9934)
- Samuel Desta Guma
- Hongjian Qin (ORCID: https://orcid.org/0009-0007-5287-8762)
- Emmanuel Mintah Bonku (ORCID: https://orcid.org/0000-0001-9333-0129)
- Farukh Sharopov (ORCID: https://orcid.org/0000-0003-0378-8887)
- Sodik Numonov (ORCID: https://orcid.org/0000-0003-4597-4047)
- Fuqiang Zhu (ORCID: https://orcid.org/0000-0001-9075-6474)
- Safomuddin Abduahadi (ORCID: https://orcid.org/0000-0001-9553-8302)
- Jun Lin
Institutions
- Academy of Sciences of the Republic of Tajikistan (TJ)
- Shanghai Institute of Materia Medica (CN)
- Shanghai Zhangjiang Laboratory (CN)
- University of Chinese Academy of Sciences (CN)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2025-12-03
- DOI
- https://doi.org/10.1021/acs.joc.5c01896
- Citations
- 1
- Primary Topic
- Synthesis of heterocyclic compounds
- Type
- article
- Field-Weighted Citation Impact
- 0.94