Abstract: We here reported a process for synthesis of avibactam sodium in kilogram scale by drug design. High purity oxalate was synthesized from L-pyroglutamic acid by esterification, tert-butoxycarbonyl protection, sulfur ylide ring opening, condensation of benzyloxyamine hydrochloride, de-tert-butoxycarbonyl, synthesis of piperidine ring, construction of the chiral carbon in position 5, isomer resolution. Oxalate gets avibactam sodium through ammonolysis, intramolecular urealization, debenzylation, sulfonic acid esterification, quaternary ammonium salt and sodium ion exchange reaction. The process not only involves mild reaction conditions, easy work-up methods, but also has a greener process. The total yield of avibactam sodium in kilogram scale was 19.7％, and HPLC purity 99.8％.