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

Abstract 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(CH 3 CN) 4 ]PF 6 as Cu(I) source.