Aza-analog of the basic disaccharide unit in heparan sulfate was designed as a potential inhibitor against heparanase produced by solid tumor cells, and synthesized via a coupling reaction of a phenyl 2-azido-1-thio-D-glucopyranoside derivative with a partially protected 1-deoxynojirymycin derived from D-glucose, followed by manipulation such as imino acid formation, O-sulfation.