ArticleChemistry (Weinheim an der Bergstrasse, Germany)2018
Synthesis of Structurally Diverse N-Substituted Quaternary-Carbon-Containing Small Molecules from α,α-Disubstituted Propargyl Amino Esters.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 26 citations in OpenAlex.
- Diastereoconvergent synthesis ofChemical science · 2022Article
- Practical asymmetric amine nucleophilic approach for the modular construction of protected α-quaternary amino acids.Chemical science · 2022Article
- Design and Synthesis of 56 Shape-Diverse 3D Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 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
- 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
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
N-containing quaternary stereocenters represent important motifs in medicinal chemistry. However, due to their inherently sterically hindered nature, they remain underrepresented in small molecule screening collections. As such, the development of synthetic routes to generate small molecules that incorporate this particular feature are highly desirable. Herein, we describe the diversity-oriented synthesis (DOS) of a diverse collection of structurally distinct small molecules featuring this three-dimensional (3D) motif. The subsequent derivatisation and the stereoselective synthesis exemplified the versatility of this strategy for drug discovery and library enrichment. Chemoinformatic analysis revealed the enhanced sp
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Registered trials
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