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Efficient Syntheses of 1,2,3-Triazoloamide Derivatives Using Solid- and Solution-Phase Synthetic Approaches
Efficient Syntheses of 1,2,3-Triazoloamide Derivatives Using Solid- and Solution-Phase Synthetic Approaches
- Source :
- Molecules, Vol 20, Iss 11, Pp 19984-20013 (2015), Molecules; Volume 20; Issue 11; Pages: 19984-20013, Molecules, Volume 20, Issue 11, Pages 19984-20013
- Publication Year :
- 2015
- Publisher :
- MDPI AG, 2015.
-
Abstract
- Efficient synthetic routes for the preparation of secondary and tertiary 1,2,3-triazoloamide derivatives were developed. A secondary α-1,2,3-triazoloamide library was constructed and expanded by a previously developed solid-phase synthetic route and a tertiary 1,2,3-triazoloamide library was constructed by a parallel solution-phase synthetic route. The synthetic routes rely on amide formation with secondary amines and chloro-acid chlorides<br />SN2 reaction with sodium azide<br />and the selective [3 + 2] Hüisgen cycloaddition with appropriate terminal alkynes. The target secondary and tertiary 1,2,3-triazoloamide derivatives were obtained with three-diversity points in excellent overall yields and purities using the reported solid- and solution-phase synthetic routes, respectively.
- Subjects :
- solid-phase synthesis
Pharmaceutical Science
1,2,3-triazoloamide
Chemistry Techniques, Synthetic
Article
Analytical Chemistry
lcsh:QD241-441
chemistry.chemical_compound
Solid-phase synthesis
lcsh:Organic chemistry
Amide
Drug Discovery
Spectroscopy, Fourier Transform Infrared
Solid-Phase Synthesis Techniques
Organic chemistry
Physical and Theoretical Chemistry
Amines
Nuclear Magnetic Resonance, Biomolecular
Organic Chemistry
solution-phase synthesis
Solution phase
Combinatorial chemistry
Cycloaddition
chemistry
Chemistry (miscellaneous)
Molecular Medicine
SN2 reaction
Sodium azide
Solution phase synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 20
- Issue :
- 11
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....b3aff33070aa428de253de1aa792b7e5