Synthesis of Enantiomerically Pure α-[4-(1-Substituted)-1,2,3-triazol-4-yl]-benzylacetamides via Microwave-Assisted Click Chemistry: Towards New Potential Antimicrobial Agents.

Abstract Chiral 1-phenyl-2-propynylamines are important building blocks for the synthesis of antifungal and antiaromatase agents related to bifonazole. In this report, a microwave-assisted Cu(I)-catalyzed ‘click chemistry’ approach has been employed to easily generate a small library of enantiomerically pure α-[4-(1-substituted)-1,2,3-triazol-4-yl]benzylacetamides starting from racemic propargylamines. These compounds could represent easily accessible intermediates for the synthesis of new antimicrobial agents.