ArticleScience (New York, N.Y.)2016
Organic chemistry. Strain-release amination.
Article in Science (New York, N.Y.), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 145 papers.
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Who cites it
145 citing papers in PubMed.
- Practical synthesis of 3-Oxa/Aza-bicyclo[3.1.1]heptanes from 3-Oxa/Aza[3.1.1]propellanes.Nature communications · 2026Article
- Visible light-mediated Alder-ene reaction of bicyclobutanes with cyclohexynes to access skipped dienes and skeletal remodeling to tetralines.Nature communications · 2026Article
- Copper-catalysed site-selective arylation of pyrazoles.Nature chemistry · 2026Article
- Methyl on the Bridge: 2-Methyl Propellane as Precursor for 1,3-Substituted 2-Methylated Bicyclo[1.1.1]Pentanes.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- PhotocatalyticOrganic letters · 2026Article
- Collective synthesis of 1,2,4-trisubstituted, meta- and ortho-substituted arene bioisosteres from bicyclobutanes.Nature chemistry · 2026Article
- Dimerisation of aryl-substituted bicyclobutanes (BCBs): revealing a new mode of 1,3-dipolar background reactivity.Chemical science · 2026Article
- Bridged scaffold editing of carbocycles and heterocycles.Nature communications · 2026Article
- Enantioselective Pyrazole Alkylation via Iridium and Squaramide Catalyzed N-H Insertion.Journal of the American Chemical Society · 2026Article
- Regio- and Stereoselective Deprotonation and Functionalization of Strained 1-Aza[n.1.0]bicycles.Journal of the American Chemical Society · 2026Article
- Lewis Acid Catalyzed Dual Strain-Release Platform for Transforming Azabicyclo[1.1.0]butanes into Functionalized Azetidines with Donor-Acceptor(D-A) Cyclopropanes and Bicyclo[1.1.0]butanes.Organic letters · 2026Article
- Attempts to Achieve Targeted Covalent Inhibition of Hsp90β.Chemical biology & drug design · 2026Article
- Introducing the heterocyclic[3.1.1]propellanes.Nature chemistry · 2026Article
- Hetero[3.1.1]propellanes.Nature chemistry · 2026Article
- Triplet Energy Transfer-Driven Intermolecular [2+2] Photocycloaddition of Acyclic Imines and Indoles: Facile Access to Azetidine-Fused Indolines.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Electrochemical Activation of Bicyclo[1.1.0]butanes.Organic letters · 2026Article
- Catalytic asymmetric functionalization of bicyclo[1.1.0]butane boronic esters enabled by 1,2-oxygen migration.Nature communications · 2026Article
- Photochemical thiocarbonyl difluoride generation enables azetidine synthesis.Nature communications · 2026Article
- Thermal [2+2] cycloaddition as a route to gem-difluoro heterobicyclo[n.1.1]alkanes.Nature chemistry · 2026Article
- Propellane-free access to bicyclo[1.1.1]pentanes.Nature communications · 2026Review
85 more citing papers are in PubMed but not listed here.
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14 authors.
Funding
Abstract
To optimize drug candidates, modern medicinal chemists are increasingly turning to an unconventional structural motif: small, strained ring systems. However, the difficulty of introducing substituents such as bicyclo[1.1.1]pentanes, azetidines, or cyclobutanes often outweighs the challenge of synthesizing the parent scaffold itself. Thus, there is an urgent need for general methods to rapidly and directly append such groups onto core scaffolds. Here we report a general strategy to harness the embedded potential energy of effectively spring-loaded C-C and C-N bonds with the most oft-encountered nucleophiles in pharmaceutical chemistry, amines. Strain-release amination can diversify a range of substrates with a multitude of desirable bioisosteres at both the early and late stages of a synthesis. The technique has also been applied to peptide labeling and bioconjugation.
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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.