ArticleAngewandte Chemie (International ed. in English)2016
Partially Saturated Bicyclic Heteroaromatics as an sp(3) -Enriched Fragment Collection.
Article in Angewandte Chemie (International ed. in English), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Couple-close: Unified approach to semisaturated cyclic scaffolds.Science (New York, N.Y.) · 2026Article
- Chiral hypervalent iodine catalyzed stereoselective skeletal editing of pyrimidine fused heterocycles.Nature communications · 2025Article
- Discovery and Development of an Aerobic Radical Hydroxyarylation Reaction Using Aryl Halides, Olefins, and OOrganic letters · 2025Article
- Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines.Communications chemistry · 2023Article
- Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates.RSC medicinal chemistry · 2022Article
- Photocatalytic Hydroaminoalkylation of Styrenes with Unprotected Primary Alkylamines.Journal of the American Chemical Society · 2021Article
- Metal Complexes for Therapeutic Applications.Trends in chemistry · 2021Article
- Rate Dependence on Inductive and Resonance Effects for the Organocatalyzed Enantioselective Conjugate Addition of Alkenyl and Alkynyl Boronic Acids to β-Indolyl Enones and β-Pyrrolyl Enones.Molecules (Basel, Switzerland) · 2021Article
- Emergent synthetic methods for the modular advancement of spChemical science · 2021Review
- Fragment-based drug discovery: opportunities for organic synthesis.RSC medicinal chemistry · 2020Review
- Design and Synthesis of 56 Shape-Diverse 3D Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Evaluation of 3-Dimensionality in Approved and Experimental Drug Space.ACS medicinal chemistry letters · 2020Article
- Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.Chemical science · 2020Article
- Cycloaddition Strategies for the Synthesis of Diverse Heterocyclic Spirocycles for Fragment-Based Drug Discovery.European journal of organic chemistry · 2019Article
- Visible-Light Photocatalytic Difluoroalkylation-Induced 1, 2-Heteroarene Migration of Allylic Alcohols in Batch and Flow.The Journal of organic chemistry · 2018Article
- Synthesis of Structurally Diverse N-Substituted Quaternary-Carbon-Containing Small Molecules from α,α-Disubstituted Propargyl Amino Esters.Chemistry (Weinheim an der Bergstrasse, Germany) · 2018Article
- Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections.Frontiers in chemistry · 2018Review
- Synthesis and Demonstration of the Biological Relevance of spChemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Divergent Synthesis of Cyclopropane-Containing Lead-Like Compounds, Fragments and Building Blocks through a Cobalt Catalyzed Cyclopropanation of Phenyl Vinyl Sulfide.European journal of organic chemistry · 2017Article
- Divergent Synthesis and Real-Time Biological Annotation of Optically Active Tetrahydrocyclopenta[c]pyranone Derivatives.Organic letters · 2016Article
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7 authors.
Funding
Abstract
Fragment-based lead generation has proven to be an effective means of identifying high-quality lead compounds for drug discovery programs. However, the fragment screening sets often used are principally comprised of sp(2) -rich aromatic compounds, which limits the structural (and hence biological) diversity of the library. Herein, we describe strategies for the synthesis of a series of partially saturated bicyclic heteroaromatic scaffolds with enhanced sp(3) character. Subsequent derivatization led to a fragment collection featuring regio- and stereo-controlled introduction of substituents on the saturated ring system, often with formation of new stereocenters.
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