Rh(III)-catalyzed C−H activation/annulation of fluoroalkylated benzhydrylamines with diarylalkynes enabled by amino directing groups

Ryu Tadano; Takeshi Yasui; Yoshihiko Yamamoto

doi:10.1016/j.tchem.2026.100160

April 1, 2026Tetrahedron ChemOpen Access

Rh(III)-catalyzed C−H activation/annulation of fluoroalkylated benzhydrylamines with diarylalkynes enabled by amino directing groups

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Key Points

The central aim is to develop a method for C−H activation and annulation using fluoroalkylated benzhydrylamines.
Utilized Cp*Rh(III) as a catalyst.
Implemented N-based directing groups to facilitate reactions.
Performed reactions with diarylalkynes to form new compounds.
Successfully synthesized fluoroalkylated dihydroisoquinolines.
Demonstrated improved efficacy in C−H activation compared to prior methods.

Implication

Demonstrates C−H activation in fluoroalkylated benzhydrylamines, indicating potential for drug discovery.

Abstract

Abstract Fluoroalkyl groups hinder C−H activation due to steric and electronic effects. This study develops N-based directing groups that enable Cp*Rh(III)-catalyzed C−H activation/annulation of fluoroalkylated benzhydrylamines with alkynes, giving fluoroalkylated dihydroisoquinolines—promising scaffolds for drug discovery.

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Cite This Study

Tadano et al. (2026) studied this question.

synapsesocial.com/papers/69d34cee9c07852e0af9733b https://doi.org/10.1016/j.tchem.2026.100160

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Rh(III)-catalyzed C−H activation/annulation of fluoroalkylated benzhydrylamines with diarylalkynes enabled by amino directing groups

Key Points

Implication

Abstract

Discussion

Cite This Study

Rh(III)-catalyzed C−H activation/annulation of fluoroalkylated benzhydrylamines with diarylalkynes enabled by amino directing groups

Key Points

Implication

Abstract

Discussion

Cite This Study

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