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A versatile synthesis of fused triazolo derivatives by sequential Ugi/alkyne-azide cycloaddition reactions
Authors:Irini Akritopoulou-Zanze  Vijaya Gracias  Stevan W. Djuric
Affiliation:Scaffold-Oriented Synthesis, Abbott Laboratories, R4CP, AP10, 100 Abbott Park Road, Abbott Park, IL 60064-6099, USA
Abstract:We report a facile synthesis of fused dihydrotriazolo[1,5-a]pyrazinones and triazolobenzodiazepines by an Ugi/alkyne-azide cycloaddition synthetic sequence. The coupling of the Ugi multi-component reaction with the intramolecular alkyne-azide cycloaddition provides access to highly functionalized heterocyclic ring systems in two steps from easily available starting materials in excellent overall yields.
Keywords:Multi-component reactions   Ugi   Intramolecular azide-alkyne cycloaddition   Fused triazolo derivatives   Dihydrotriazolo[1,5-a]pyrazinones   Triazolobenzodiazepines   Sequential Ugi/IAAC   Fused heterocycles
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