Synthesis of <i>N</i> -Unsubstituted 1-Aminoisoquinolines via Rh(III)-Catalyzed C–H Activation/Annulation of Benzamidine Hydrochloride with Diazo Compounds
An efficient protocol for the synthesis of <i>N</i>-unsubstituted 1-aminoisoquinolines via Rh(III)-catalyzed C-H cascade annulation using benzamidine hydrochloride and α-diazocarbonyl compounds has been presented. A series of <i>N</i>-unsubstituted 1-aminoisoquinolines can be obtained in moderate-to-good yields from this reaction, which features broad functional group tolerance. Moreover, large-scale reaction and further synthetic transformation of the desired product were conducted to demonstrate the potential utility of this annulation.
Authors
- Baoheng Wu
- Wei Zhou (ORCID: https://orcid.org/0000-0001-9817-0646)
- Ye Tian (ORCID: https://orcid.org/0000-0002-9168-6954)
- Ning Xu (ORCID: https://orcid.org/0000-0002-4613-2151)
- Tao Chen (ORCID: https://orcid.org/0000-0003-4392-3748)
- He Li (ORCID: https://orcid.org/0000-0003-3588-0215)
- Ye Lu (ORCID: https://orcid.org/0000-0003-4995-5265)
- Jinglin Liu (ORCID: https://orcid.org/0000-0001-6361-7380)
- Deshuai Huang
- Zhixiang Lu
- Tianyi Liu
- Botong Sun
- Liang Xu
Institutions
- Laboratoire de physique des Solides (FR)
- Ministry of Education (IR)
- National University of Mongolia (MN)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2026-03-13
- DOI
- https://doi.org/10.1021/acs.joc.5c02907
- Primary Topic
- Catalytic C–H Functionalization Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.00