Enantioselective Hydrogenation of Benzofurans with Water <i>via</i> Rh/Hf Cooperative Catalysts: Convenient Access to Chiral 2,3‐Dihydrobenzofurans
Comprehensive Summary The chiral 2,3‐dihydrobenzofuran (DHB) scaffold is a privileged motif in bioactive natural products and preclinical therapeutic candidates, yet practical enantioselective syntheses remain scarce. We report a chiral Rh/Hf/( S )‐DTBM‐SEGPHOS bimetallic catalytic system enabling asymmetric hydrogenation of benzofurans with hydrogen source, delivering diverse DHBs (37 examples) in excellent yields (up to 98%) and enantioselectivities (up to 99% ee ). Gram‐scale synthesis and deuterium labeling with D 2 O (8 examples) validate the method's scalability and utility in biological studies and drug design.
Authors
- Baomin Fan
- Ponnam Devendar (ORCID: https://orcid.org/0000-0003-3079-1491)
- Tao Xiong (ORCID: https://orcid.org/0000-0002-5476-4036)
- Jingchao Chen (ORCID: https://orcid.org/0000-0002-6978-497X)
- Qiongtong Yang
- Hekun Yang
Institutions
- Minzu University of China (CN)
- Yunnan University (CN)
- State Ethnic Affairs Commission (CN)
Publication Details
- Journal
- Chinese Journal of Chemistry
- Published
- 2025-08-22
- DOI
- https://doi.org/10.1002/cjoc.70249
- Primary Topic
- Asymmetric Hydrogenation and Catalysis
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China
- Yunnan Provincial Science and Technology Department