Ceftizoxime alapivoxil monohydrochloride was synthesized from (6R,7R)-7-amino-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and 2-mercaptobenzothiazolyl (Z)-2-[[[(S)-2-(t-butoxycarbonyl) amino-1-oxopropyl]amine] thiazol-4-yl]-2-methoxyiminoacetate by condensation, esterification with iodomethyl pivalate, de-protection and then salt formation. The overall yield was 72%.