An Efficient Asymmetric Synthesis of Finerenone via Evans’ Chiral Auxiliary
This article reports a new application of Evans’ chiral auxiliary for an efficient asymmetric synthesis of finerenone. This new application successfully achieves the key step of stereoselective construction of the naphthyridine core of finerenone, with a high diastereomeric ratio (dr 86:14) and an 80% yield of the desired product via Evans’ chiral (R)‐4‐benzyl‐2‐oxazolidinone. The downstream transamidation of ethyl ester, with ammonia, leads to the formation of finerenone.
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)
- Feipu Yang (ORCID: https://orcid.org/0000-0003-2561-671X)
- Fuqiang Zhu (ORCID: https://orcid.org/0000-0001-9075-6474)
- Safomuddin Abduahadi (ORCID: https://orcid.org/0000-0001-9553-8302)
- Zayniddin Nuriddinov
Institutions
- Chinese Academy of Sciences (CN)
- Danaher (United States) (US)
- Xinjiang Technical Institute of Physics & Chemistry (CN)
- Shanghai Institute of Materia Medica (CN)
- Shanghai Zhangjiang Laboratory (CN)
- University of Chinese Academy of Sciences (CN)
- State Key Laboratory of Drug Research
Publication Details
- Journal
- European Journal of Organic Chemistry
- Published
- 2025-06-11
- DOI
- https://doi.org/10.1002/ejoc.202500538
- Citations
- 2
- Primary Topic
- Axial and Atropisomeric Chirality Synthesis
- Type
- article
- Field-Weighted Citation Impact
- 1.87