Synthesis of N -Unsubstituted 1-Aminoisoquinolines via Rh(III)-Catalyzed C–H Activation/Annulation of Benzamidine Hydrochloride with Diazo Compounds

The Journal of Organic Chemistry 2026

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Authors: Baoheng Wu, Ning Xu, Deshuai Huang, Tao Chen, Tianyi Liu, Zhixiang Lu, Ye Tian, Botong Sun, Ye Lu, Liang Xu, Jinglin Liu, Wei Zhou
+1 more He Li
DOI: 10.1021/acs.joc.5c02907
Cited by: 2
References: 54

Abstract

An efficient protocol for the synthesis of N -unsubstituted 1-aminoisoquinolines via Rh(III)-catalyzed C–H cascade annulation using benzamidine hydrochloride and α-diazocarbonyl compounds has been presented. A series of N -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.

Fields of Study & Subjects

Catalytic C–H Functionalization Methods Cyclopropane Reaction Mechanisms Catalytic Alkyne Reactions

Publication details

Journal / source
The Journal of Organic Chemistry
Publisher
American Chemical Society (ACS)
Volume
91
Issue
12
Pages
4502–4507
Publication date
13 March 2026
Language
EN