Solid-phase based synthesis of biologically promising triazolyl aminoacyl (peptidyl) penicillins

An efficient and versatile methodology for the preparation of valuable triazolyl aminoacyl (peptidyl) penicillins is described. Solid-phase Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition was used as the key step showing general applicability and excellent regioselectivity either with CuI or [Cu(CH3CN)(4)]PF6 as Cu(I) source. (C) 2011 Elsevier Ltd. All rights reserved.