ArticleJACS Au2022
Merging Directed C-H Activations with High-Throughput Experimentation: Development of Iridium-Catalyzed C-H Aminations Applicable to Late-Stage Functionalization.
Article in JACS Au, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed.
- AI-driven nanomedicine for cancer theranostics.Molecular cancer · 2026Review
- Progress and future outlook towards a safe and sustainable production and use of chemicals.Communications chemistry · 2025Review
- High-Throughput Enabled Iridium-Catalyzed C-H Borylation Platform for Late-Stage Functionalization.ACS catalysis · 2025Article
- Synthesis of Benzoic Acids from Electrochemically Reduced COChemSusChem · 2025Article
- Late-stage meta-C-H alkylation of pharmaceuticals to modulate biological properties and expedite molecular optimisation in a single step.Nature communications · 2024Article
- Late-stage synthesis of heterobifunctional molecules for PROTAC applications via ruthenium-catalysed C‒H amidation.Nature communications · 2023Article
- A Brief Introduction to Chemical Reaction Optimization.Chemical reviews · 2023Review
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Herein, we report an iridium-catalyzed directed C-H amination methodology developed using a high-throughput experimentation (HTE)-based strategy, applicable for the needs of automated modern drug discovery. The informer library approach for investigating the accessible directing group chemical space, in combination with functional group tolerance screening and substrate scope investigations, allowed for the generation of reaction application guidelines to aid future users. Applicability to late-stage functionalization of complex drugs and natural products, in combination with multiple deprotection protocols leading to the desirable aniline matched pairs, serve to demonstrate the utility of the method for drug discovery. Finally, reaction miniaturization to a nanomolar range highlights the opportunities for more sustainable screening with decreased material consumption.
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Registered trials
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