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.
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 / Daniele Castagnolo;Filippo Dessì;Marco Radi;Maurizio Botta. - In: TETRAHEDRON-ASYMMETRY. - ISSN 0957-4166. - 18(2007), pp. 1345-1350. [10.1016/j.tetasy.2007.06.007]