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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

Authors :
Jong-Sup Bae
Joobin Kim
Chang-Woo Cho
Doohyun Lee
Youn Kyung Son
Dong Jae Baek
Kwang-Hyeon Liu
Daehun Kim
Taegeum Kim
Tae-Ho Lee
Kyung-Sik Song
Sohee Kim
Seungyeon Lee
Sangkyu Lee
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.

Details

Language :
English
ISSN :
14203049
Volume :
20
Issue :
11
Database :
OpenAIRE
Journal :
Molecules
Accession number :
edsair.doi.dedup.....b3aff33070aa428de253de1aa792b7e5