Synthesis of Structurally Diverse N-Substituted Quaternary-Carbon-Containing Small Molecules from α,α-Disubstituted Propargyl Amino Esters

Autor:	Natalia, Mateu, Sarah L, Kidd, Leen, Kalash, Hannah F, Sore, Andrew, Madin, Andreas, Bender, David R, Spring
Rok vydání:	2018
Předmět:	molecular diversity Full Paper medicinal chemistry quaternary stereocenters Full Papers Synthetic Methods diversity-oriented synthesis human activities drug discovery
Zdroj:	Chemistry (Weinheim an Der Bergstrasse, Germany)
ISSN:	1521-3765
Popis:	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 sp3 character of the target library and demonstrated that it represents an attractive collection of biologically diverse small molecules with high scaffold diversity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::9db45614deaa7340cb94c773b5f19a2a https://pubmed.ncbi.nlm.nih.gov/30011115 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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