Allyl 4-O-{3-deoxy-3-[4-benzylaminocarbonyl-1H-（1,2,3）-triazol-1-yl]-β-D-galactopyranosyl}-2-deoxy-2-acetamido- β-D-glucopyranoside, a potential inhibitor of galectin-3, was designed and synthesized using lactose as stating material. The modifications of lactose included in introducing of N-acetamino group at the C-2 position through an azidoiodoglycosylation meanwhile constructing the [3-aminolactoside stereoselectively and replacing 3＇-OH with substituent 1,2,3-triazolyl group to enhance the affinity toward galeetin-3.
