Efficient Syntheses of 1,2,3-Triazoloamide Derivatives Using Solid- and Solution-Phase Synthetic Approaches

Area of Science:

• Organic Chemistry
• Medicinal Chemistry

Background:

• 1,2,3-triazoloamide derivatives are important scaffolds in medicinal chemistry.
• Development of efficient synthetic routes is crucial for library synthesis.

Purpose of the Study:

• To develop efficient synthetic routes for secondary and tertiary 1,2,3-triazoloamide derivatives.
• To construct and expand secondary and tertiary 1,2,3-triazoloamide libraries.

Main Methods:

• Amide formation using secondary amines and chloro-acid chlorides.
• SN2 reaction utilizing sodium azide.
• Selective [3 + 2] Huisgen cycloaddition with terminal alkynes.

Main Results:

• Developed solid-phase and parallel solution-phase synthetic routes.
• Successfully synthesized secondary and tertiary 1,2,3-triazoloamide libraries.
• Achieved excellent overall yields and purities for target derivatives with three points of diversity.

Conclusions:

• The developed synthetic routes are efficient for preparing diverse secondary and tertiary 1,2,3-triazoloamide derivatives.
• These methods facilitate the construction of compound libraries for drug discovery and development.