METHOD FOR THE PREPARATION OF PIVALOYLOXYMETHYL ESTERS OF SULBACTAM

Pivsulbactam is an orally applied premedicamentous form of -lactamase inhibitor sulbactam and is used in the clinical practice in combination with different orally applied - lactam antibiotics, such as amplicillin, amoxicillin, and others, reducing their minimum suppressive concentrations and extending their antibacterial spectrum. By the method, pivsulbactam is produced in reaction between sulbactam-sodium salt and pivaloyloxymethylchloride in polar aprotonic solvent medium such as dimethylsulphoxide, N,N-dimethylacetamide, N,N-dimethylformamide and 1-methy-2-pyrrolidone and others at temperatures from 0 to 60°C for 18 to 24 hours in the presence or absence of sodium iodide as catalyst. The isolation of the produced pivaloyloxymethyl ester of the sulbactam is effected by the dilution of the reaction mixture with water at the end of the reaction and filtering of the drooped out crystals. By the method, slbactam pivalate is produced having 80-85% yield and over 98% purity (by the method of BETX).