Directing Group‐Assisted Rh(III)‐Catalyzed Ortho ‐Heteroarylation of Arenes via Double C─H Bond Activation

Q: What does this research mean for the field?

Rh(III)-catalyzed ortho-heteroarylation of arenes via double C-H bond activation, assisted by various directing groups, is a feasible and versatile synthetic method for forming new C-C bonds in natural products and bioactive compounds. Novelty: ClaimNovelty.SYNTHESIS. Consensus alignment: ConsensusAlignment.NEUTRAL.

Sahil Roy; Abadh Kishor Jha; Shankar Kumar; Rangnath Ravi; Karunesh Keshav; Bimal Prasad Jit

doi:10.1002/slct.74363

September 1, 2026ChemistrySelect

Directing Group‐Assisted Rh(III)‐Catalyzed Ortho ‐Heteroarylation of Arenes via Double C─H Bond Activation

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Key Points

To review directing group-assisted Rh(III)-catalyzed ortho-heteroarylation of arenes proceeding through double C─H bond activation.
Surveyed chemical literature evaluating various directing groups, such as amine-, azine-, oxime-, and thioether-derived functional groups.
Examined catalytic pathways that enable dual C─H bond cleavage and subsequent selective C─C bond formation.
Directing groups effectively coordinate Rh(III) catalysts to achieve selective ortho C─H functionalization in tandem with heteroaryl C─H activation.
Catalytic transformations demonstrated broad feasibility for the late-stage heteroarylation of natural products and bioactive scaffolds.

Implication

Review reveals mechanisms of Rh(III)-catalyzed ortho-heteroarylation across arenes, highlighting applications in functionalizing bioactive molecules.

Abstract

In this review, we have discussed the Rh(III)‐catalyzed ortho ‐heteroarylation of arenes via double C─H bond activation assisted by directing groups (DG) such as amine‐derived, azine‐derived, acid, oxime‐derived, N ‐sulfonylimine, cyanogen, azo, N ‐nitroso, thioether, and so forth, to form new C─C bonds. The synthetic methods are feasible for heteroarylation of natural products and many bioactive compounds.

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Cite This Study

Roy et al. (2026) studied this question.

synapsesocial.com/papers/6a9ab0dc5d9e33f25c631e72 https://doi.org/10.1002/slct.74363

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Directing Group‐Assisted Rh(III)‐Catalyzed Ortho ‐Heteroarylation of Arenes via Double C─H Bond Activation

Key Points

Implication

Abstract

Discussion

Cite This Study

Directing Group‐Assisted Rh(III)‐Catalyzed Ortho ‐Heteroarylation of Arenes via Double C─H Bond Activation

Key Points

Implication

Abstract

Discussion

Cite This Study

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