An expeditious approach to 1-(isoquinolin-1-yl)guanidines via a three-component reaction of 2-alkynylbenzaldehyde, sulfonohydrazide, with carbodiimide

Article abstract of DOI:10.1016/j.tet.2011.06.056

A small library of 1-(isoquinolin-1-yl)guanidine is constructed efficiently via a silver triflate-catalyzed three-component reaction of 2-alkynylbenzaldehyde, sulfonohydrazide, with carbodiimide. The preliminary biological screens of these isoquinoline library members have been evaluated, which show promising results as PTP1B inhibitor and HCT-116 inhibitor.