ReviewNature reviews. Chemistry2021
Late-stage C-H functionalization offers new opportunities in drug discovery.
Review in Nature reviews. Chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 207 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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
207 citing papers in PubMed.
- A one carbon linchpin for Rh(iii)-catalyzed, C(spOrganic chemistry frontiers : an international journal of organic chemistry · 2026Article
- An alkyl-swap platform for late-stage modification of secondary N-methylamines.Nature chemistry · 2026Article
- Interfacial Proton Ordering Near the Electrode Surface Directs Carbonyl Electroreduction to Methylene.Angewandte Chemie (International ed. in English) · 2026Article
- Base-Promoted Benzylic C-H Amination Reactions Across a Wide pKa Spectrum Enabled by 2-Halobenzofuran and -Indole Oxidants.Journal of the American Chemical Society · 2026Article
- Single-Atom Iron-Catalyzed Oxidative Esterification: From Methylarenes to the Upcycling of Polystyrene and Lignin-Derived Feedstocks.Angewandte Chemie (International ed. in English) · 2026Article
- Versatile Palladium-Catalyzed C-H Arylation of Fluoroarenes with 2-Chloropyridine Derivatives.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- A Photoredox C-H Arene Functionalization toward Substituted Methyls.Journal of the American Chemical Society · 2026Article
- Phenoxazines with a PhototransferableJournal of the American Chemical Society · 2026Article
- Deprotonative Single-Electron Oxidation as a General and Controllably Selective Platform for Benzylic C-H Functionalization.Journal of the American Chemical Society · 2026Article
- Skeletal rearrangement of [4]helicenes under acidic conditions: dynamic chirality and improved properties by subsequent peripheral editing.Chemical science · 2026Article
- Bridged scaffold editing of carbocycles and heterocycles.Nature communications · 2026Article
- Merging Micellar Catalysis and C-H Activation: Silver-Free Direct Arylation of Fluoroarenes in Water.ChemSusChem · 2026Article
- Silver-catalysed intermolecular benzylic-selective C-H amidationChemical science · 2026Article
- Asymmetric Synthesis ofJournal of the American Chemical Society · 2026Article
- Chiral S(VI) platform unifies selective C-H amination of complex molecules and alkane feedstocks.Science (New York, N.Y.) · 2026Article
- Dual Ligand-Enabled Nondirected C─H Olefination of (Hetero)Arenes for the Synthesis of Clickable Derivatives.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Highly Active CH Bond Borylation of Aromatics With Pyridine as Convenient, Low-Cost Ligand Under Iridium Catalysis.ChemSusChem · 2026Article
- Regiodivergent C3 and C4 Amination of Quinolines via Radical and Ionic Pathways.Angewandte Chemie (International ed. in English) · 2026Article
- Anomeric Amides: Valuable Reagents in Synthetic Organic Chemistry.Angewandte Chemie (International ed. in English) · 2026Review
- Efficient Approaches to Six-Membered Polyazacyclic Compounds-Part 3: C-H Functionalization of Heterocycles.Molecules (Basel, Switzerland) · 2026Review
147 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Over the past decade, the landscape of molecular synthesis has gained major impetus by the introduction of late-stage functionalization (LSF) methodologies. C-H functionalization approaches, particularly, set the stage for new retrosynthetic disconnections, while leading to improvements in resource economy. A variety of innovative techniques have been successfully applied to the C-H diversification of pharmaceuticals, and these key developments have enabled medicinal chemists to integrate LSF strategies in their drug discovery programmes. This Review highlights the significant advances achieved in the late-stage C-H functionalization of drugs and drug-like compounds, and showcases how the implementation of these modern strategies allows increased efficiency in the drug discovery process. Representative examples are examined and classified by mechanistic patterns involving directed or innate C-H functionalization, as well as emerging reaction manifolds, such as electrosynthesis and biocatalysis, among others. Structurally complex bioactive entities beyond small molecules are also covered, including diversification in the new modalities sphere. The challenges and limitations of current LSF methods are critically assessed, and avenues for future improvements of this rapidly expanding field are discussed. We, hereby, aim to provide a toolbox for chemists in academia as well as industrial practitioners, and introduce guiding principles for the application of LSF strategies to access new molecules of interest.
Identifiers
37117588What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.