Synthesis of Functionalized Bicyclic Triazoles from Chiral Aziridines

Enantiomerically pure 3-substituted-5-amino-4-hydroxy-5,6-dihydro-4H-pyrrolo[1,2-c][1,2,3]triazoles were synthesized efficiently from the sequential reactions including a regioselective ring-opening of 1-aziridine-2-yl-propargylic alcohols by azidotrimethylsilane and the subsequent intramolecular 1,3-dipolar cycloaddition between alkyne and azide.