Palladium-Catalyzed One-Pot Synthesis of 3-Arylindoles Based on <i>o</i> -Iodoaniline with Aryl Hydrazones
A tandem one-pot strategy for the efficient synthesis of indole derivatives has been developed via palladium-catalyzed coupling of <i>ortho</i>-iodoanilines with <i>N</i>-tosylhydrazones under basic conditions. The reaction proceeds through in situ formation of <i>o</i>-vinylaniline intermediates, followed by oxidative cyclization under palladium catalysis. The substrate scope study provided substituted 3-phenylindoles in moderate to good yields, demonstrating the method's practicality for indole construction. Notably, no protection of the indole N-H is required, representing a key advantage.
Authors
- Yu Liu (ORCID: https://orcid.org/0000-0003-2608-6941)
- Tengfei Zhang (ORCID: https://orcid.org/0000-0002-5978-3818)
- Yue Chen (ORCID: https://orcid.org/0000-0001-6604-7221)
- Dong‐Sheng Chen (ORCID: https://orcid.org/0000-0002-1738-1896)
- Zhihao Du (ORCID: https://orcid.org/0009-0007-5125-8473)
Institutions
- Institute for Student Achievement (US)
- Shanghai Institute of Pharmaceutical Industry (CN)
Publication Details
- Journal
- ACS Omega
- Published
- 2025-11-16
- DOI
- https://doi.org/10.1021/acsomega.5c07730
- Primary Topic
- Catalytic C–H Functionalization Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.00