ReviewNature chemistry2018
Organic synthesis provides opportunities to transform drug discovery.
Review in Nature chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 431 papers.
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Who cites it
431 citing papers in PubMed.
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- Organophosphine-mediated formal [4 + 2] cycloadditions of benzo[c][1,2]dithiol-3-ones and iso(thio)cyanates via S to C-N skeletal editing strategy.Molecular diversity · 2026Article
- Cobalt-Catalyzed Reductive Asymmetric Dimerization of 1,3-Enynes: Rapid Synthesis of Enantioenriched Skipped 1,3,6-Trienes.Angewandte Chemie (International ed. in English) · 2026Article
- Modular Assembly of Bioconjugates Enabled by a Pyridine-Based Chemoselective Sequential Conjugation Platform.Angewandte Chemie (International ed. in English) · 2026Article
- Remapping the Synthetic Landscape of α-Tertiary Alkylamines via Dual-Functional Catechol.Angewandte Chemie (International ed. in English) · 2026Article
- Article
- A General Photoredox Platform for the Hydroarylation of Olefins.Journal of the American Chemical Society · 2026Article
- Photochemical Synthesis of β‑N-Heterocycle Alcohols via a Coordination-Induced 1,5-Boronate Sigmatropic Rearrangement.JACS Au · 2026Article
- Nitrene generation and transfer for unnatural biosynthesis in living cells.Nature chemistry · 2026Article
- Base-Free C-N Cross-Electrophile Coupling.Journal of the American Chemical Society · 2026Article
- Formal Markovnikov Hydroazolation of Alkenes via Reductive Activation of Alkylthianthrenium Salts.Journal of the American Chemical Society · 2026Article
- Formal Hydride Abstraction: A Unified Photoredox Platform for Nucleophilic C(sp3)-H Functionalization.Accounts of chemical research · 2026Article
- Copper-catalysed site-selective arylation of pyrazoles.Nature chemistry · 2026Article
- Direct Stereospecific Deoxyamination of Alcohols Enabled by Li-Mediated SuFEx.Organic letters · 2026Article
- Carbonylative Aminative Suzuki-Miyaura Coupling: Pd-Catalyzed Synthesis of Amides from Vinyl/Aryl Halides and Boronic Acids.Journal of the American Chemical Society · 2026Article
- Lactam Framework Editing via Formal Methylene Deletion.Journal of the American Chemical Society · 2026Article
- Nitrogen atom insertion and related skeletal editing strategies in aromatic heterocycles for drug discovery (2015-2025).Molecular diversity · 2026Review
- A photochemical strategy for pyrazole to imidazole conversion.Chemical science · 2026Article
- Decarboxylative carbonyl alkylative amination: A general and practical strategy for aliphatic amine synthesis.Science advances · 2026Article
- Shape-Conserving Atom Replacements.Chemical reviews · 2026Review
371 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Despite decades of ground-breaking research in academia, organic synthesis is still a rate-limiting factor in drug-discovery projects. Here we present some current challenges in synthetic organic chemistry from the perspective of the pharmaceutical industry and highlight problematic steps that, if overcome, would find extensive application in the discovery of transformational medicines. Significant synthesis challenges arise from the fact that drug molecules typically contain amines and N-heterocycles, as well as unprotected polar groups. There is also a need for new reactions that enable non-traditional disconnections, more C-H bond activation and late-stage functionalization, as well as stereoselectively substituted aliphatic heterocyclic ring synthesis, C-X or C-C bond formation. We also emphasize that syntheses compatible with biomacromolecules will find increasing use, while new technologies such as machine-assisted approaches and artificial intelligence for synthesis planning have the potential to dramatically accelerate the drug-discovery process. We believe that increasing collaboration between academic and industrial chemists is crucial to address the challenges outlined here.
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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.