Synthesis of Benzo[3,4]azepino[1,2‐ a ]indoles via Rh (III)‐Catalyzed NH ‐Indole‐Directed C‐H/N‐H [4+3] Annulation of 2‐Phenylindoles With Methyleneoxetanones

Applied Organometallic Chemistry 2026

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Authors: Piao Lu, Siqi Zhang, Leipeng Lu, Xinlu Xu, Qiufeng Huang
DOI: 10.1002/aoc.70520
Cited by: 1
References: 75

Abstract

ABSTRACT A regioselective rhodium‐catalyzed NH ‐indole‐directed C–H coupling of 2‐arylindoles with methyleneoxetanones, followed by TsCl/DMAP‐mediated intramolecular amidation leading to biologically relevant benzo[3,4]azepino[1,2‐ a ]indoles bearing a fused seven‐membered ring is presented. Excellent functional group tolerance is demonstrated, yielding diverse indole‐fused seven‐membered‐ring architectures and providing gramme quantities of products through scalability.

Fields of Study & Subjects

Catalytic C–H Functionalization Methods Cyclopropane Reaction Mechanisms Catalytic Cross-Coupling Reactions

Publication details

Journal / source
Applied Organometallic Chemistry
Publisher
Wiley
Volume
40
Issue
2
Publication date
15 January 2026
Language
EN