ArticleJournal of the American Chemical Society2017
Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity.
Article in Journal of the American Chemical Society, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 88 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
88 citing papers in PubMed, 332 citations in OpenAlex.
- Visible light-mediated Alder-ene reaction of bicyclobutanes with cyclohexynes to access skipped dienes and skeletal remodeling to tetralines.Nature communications · 2026Article
- Catalytic Transformations of Aza-Cyclobutenes, Fused Cyclobutenes, and Cyclobutenones.Chemical record (New York, N.Y.) · 2026Review
- A Scalable Stereoselective Synthesis of Polysubstituted Housanes.Organic letters · 2026Article
- Dimerisation of aryl-substituted bicyclobutanes (BCBs): revealing a new mode of 1,3-dipolar background reactivity.Chemical science · 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
- Stereocontrolled Synthesis of Polysubstituted Housanes viaJournal of the American Chemical Society · 2026Article
- Attempts to Achieve Targeted Covalent Inhibition of Hsp90β.Chemical biology & drug design · 2026Article
- Electrochemical Activation of Bicyclo[1.1.0]butanes.Organic letters · 2026Article
- Photochemical thiocarbonyl difluoride generation enables azetidine synthesis.Nature communications · 2026Article
- How topology governs cation affinity: protonation and metal coordination in 1- and 9-azahomocubane.RSC advances · 2026Article
- Photochemical Construction of Trifluoromethyl Bicyclo[1.1.1]pentyl-heterocycles.Organic letters · 2026Article
- Boron-Enabled Stereoselective Synthesis of Polysubstituted Housanes.Journal of the American Chemical Society · 2025Article
- Article
- HFIP-assisted Brønsted acid-catalyzed ring opening of 1-azabicyclo[1.1.0]butane to access diverse C3-quaternary aza-azetidines and indole-azetidines.Nature communications · 2025Article
- Diastereoselective synthesis of multi-substituted cyclobutanes via catalyst-controlled regiodivergent hydrophosphination of acyl bicyclobutanes.Nature communications · 2025Article
- Highly stereoselective synthesis of polysubstituted housanes and spiro-oxa-housanes: application and mechanistic insights.Chemical science · 2025Article
- Regiodivergent hydrophosphination of Bicyclo[1.1.0]-Butanes under catalyst control.Nature communications · 2025Article
- Enantiocontrolled Azetidine Library Synthesis via Strain-Release Functionalization of 1-Azabicyclobutanes.Journal of the American Chemical Society · 2025Article
- Synthesis of 2-(Trifluoromethyl)Azetidines by Strain-Release Reactions of 2-(Trifluoromethyl)-1-Azabicyclo[1.1.0]Butanes.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Article
28 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
24 authors at 3 institutions in 1 country.
Funding
Abstract
Driven by the ever-increasing pace of drug discovery and the need to push the boundaries of unexplored chemical space, medicinal chemists are routinely turning to unusual strained bioisosteres such as bicyclo[1.1.1]pentane, azetidine, and cyclobutane to modify their lead compounds. Too often, however, the difficulty of installing these fragments surpasses the challenges posed even by the construction of the parent drug scaffold. This full account describes the development and application of a general strategy where spring-loaded, strained C-C and C-N bonds react with amines to allow for the "any-stage" installation of small, strained ring systems. In addition to the functionalization of small building blocks and late-stage intermediates, the methodology has been applied to bioconjugation and peptide labeling. For the first time, the stereospecific strain-release "cyclopentylation" of amines, alcohols, thiols, carboxylic acids, and other heteroatoms is introduced. This report describes the development, synthesis, scope of reaction, bioconjugation, and synthetic comparisons of four new chiral "cyclopentylation" reagents.
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What 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.