期刊
MOLECULES
卷 20, 期 11, 页码 19984-20013出版社
MDPI AG
DOI: 10.3390/molecules201119673
关键词
1,2,3-triazoloamide; solid-phase synthesis; solution-phase synthesis
资金
- National Research Foundation of Korea (NRF) from the Basic Science Research Program, the Ministry of Science, ICT and Future Planning, Republic of Korea [NRF-2014R1A1A1037635, NRF-2014R1A2A1A11052798]
- Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI) - Ministry of Health & Welfare, Republic of Korea [HI11C1300(A111345)]
Efficient synthetic routes for the preparation of secondary and tertiary 1,2,3-triazoloamide derivatives were developed. A secondary -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; S(N)2 reaction with sodium azide; and the selective [3 + 2] Huisgen 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.
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