What question did this study set out to answer?

This research focuses on developing a protocol for synthesizing N-unsubstituted 1-aminoisoquinolines.

March 15, 2026

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

Key Points

This research focuses on developing a protocol for synthesizing N-unsubstituted 1-aminoisoquinolines.
Conducted Rh(III)-catalyzed C-H cascade annulation with benzamidine hydrochloride and diazo compounds.
Tested broad functional group tolerance in the synthesis process.
Performed large-scale reactions to assess practicality.
Achieved moderate-to-good yields of N-unsubstituted 1-aminoisoquinolines.
Demonstrated potential for further synthetic transformations of products.

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.

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