Enantioselective Synthesis of Indole-Derived Atropisomers through Rh(I)-Catalyzed C–H Arylation with Aryl Bromides
A Rh(I)-catalyzed enantioselective C2-arylation of indole derivatives with aryl bromides is reported. In the presence of the Rh/chiral cyclohexyl-fused SPINOL-derived phosphoramidite complex, C2-arylation of indoles proceeded smoothly, affording a wide range of indole-C3 biaryl-type atropisomers in good yields and enantioselectivity (up to 98% yield, up to 92% ee) under mild conditions. This method displays good functional group tolerance.
Authors
- Qiansujia Zhou
- Chen‐Xu Liu (ORCID: https://orcid.org/0009-0007-4793-0984)
- Fangnuo Zhao
- Chongqing Pan (ORCID: https://orcid.org/0000-0002-8667-6049)
- Si‐Yong Yin
- Shu-Li You (ORCID: https://orcid.org/0000-0003-4586-8359)
- Qing Gu (ORCID: https://orcid.org/0000-0003-4963-2271)
- Yu-Shan Zheng
Institutions
- Shanghai Institute of Organic Chemistry (CN)
- University of Chinese Academy of Sciences (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2026-05-22
- DOI
- https://doi.org/10.1021/acs.orglett.6c01540
- Primary Topic
- Axial and Atropisomeric Chirality Synthesis
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China
- Science and Technology Commission of Shanghai Municipality
- National Key Research and Development Program of China