DNA-Compatible Synthesis of α,β-Epoxyketones for DNA-Encoded Chemical Libraries.
Sign Up to like & getrecommendations! Published in 2021 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.1c00567
Abstract: As a powerful platform in drug discovery, the DNA-encoded chemical library technique enables the generation of numerous chemical members with high structural diversity. Epoxides widely exist in a variety of approved drugs and clinical candidates,… read more here.
Keywords: dna; dna encoded; dna compatible; compatible synthesis ... See more keywords
DNA Compatible Oxidization and Amidation of Terminal Alkynes.
Sign Up to like & getrecommendations! Published in 2022 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.2c00340
Abstract: Through a modified Kinugasa reaction, a novel method of amidation on terminal oligo alkyne conjugates by copper-promoted oxidation with nitrones has been developed. Unprotected bifunctional carboxylic acid-amine reagents can be transformed directly to the respective… read more here.
Keywords: amidation terminal; dna compatible; compatible oxidization; terminal alkynes ... See more keywords
DNA-Compatible Nitro Reduction and Synthesis of Benzimidazoles.
Sign Up to like & getrecommendations! Published in 2022 at "Methods in molecular biology"
DOI: 10.1021/acs.bioconjchem.7b00416.s001
Abstract: A key factor for productive DNA-encoded libraries is the chemical diversity of the small molecule moiety attached to an encoding DNA oligomer. The library structure diversity is often limited to DNA-compatible chemical reactions in aqueous… read more here.
Keywords: dna compatible; benzimidazoles dna; synthesis benzimidazoles; compatible nitro ... See more keywords
DNA Compatible Intermolecular Wittig Olefination for the Construction of α, β-Unsaturated Carbonyl Compounds.
Sign Up to like & getrecommendations! Published in 2020 at "Organic letters"
DOI: 10.1021/acs.orglett.0c01215
Abstract: A robust DNA-compatible Wittig reaction mediated by PPh2CH3 has been validated for DNA-conjugated α-chloroacetamides with aldehydes and, alternatively, DNA-conjugated aldehydes with α-halo acetamides or ketones. Further, 2-aminopyridines were acylated with α-chloroacetyl chloride and then reacted… read more here.
Keywords: dna compatible; carbonyl compounds; compatible intermolecular; unsaturated carbonyl ... See more keywords
Multicomponent DNA-Compatible Synthesis of an Annelated Benzodiazepine Scaffold for Focused Chemical Libraries.
Sign Up to like & getrecommendations! Published in 2023 at "Organic letters"
DOI: 10.1021/acs.orglett.2c04293
Abstract: Annelated benzodiazepines are attractive drug-like scaffolds with a broad spectrum of biological activities. Incorporation of this heterocyclic core into DNA-encoded chemical libraries (DELs) via multicomponent assembly is highly demanded. Herein, we developed a DNA-compatible method… read more here.
Keywords: dna; dna compatible; chemical libraries; benzodiazepine ... See more keywords
The Furan-Thiol-Amine Reaction Facilitates DNA-Compatible Thiopyrrole-Grafted Macrocyclization and Late-Stage Amine Transformation.
Sign Up to like & getrecommendations! Published in 2024 at "Organic letters"
DOI: 10.1021/acs.orglett.4c04505
Abstract: We here report an efficient DNA-compatible furan-thiol-amine reaction for macrocyclization and late-stage amine transformation. This reaction, conducted under mild conditions, enables the facile cyclization of DNA-conjugated linear peptides into thiopyrrole-grafted macrocycles regardless of ring size… read more here.
Keywords: reaction; furan thiol; dna compatible; transformation ... See more keywords
DNA-Compatible Functional Group Transformations via K2RuO4-mediated Oxidation
Sign Up to like & getrecommendations! Published in 2024 at "Organic Chemistry Frontiers"
DOI: 10.1039/d4qo00203b
Abstract: Functional group transformation represents a potent strategy for enriching the chemical diversity in DNA-encoded chemical library (DEL) synthesis. Within the realm of functional group transformation reactions, oxidation stands out as... read more here.
Keywords: group transformations; functional group; transformations via; compatible functional ... See more keywords