摘要 |
NEW MATERIAL:An azetidinone derivative shown by the formula I (R1 is acyl, H, or amino-protecting group; X is H, alkyloxy, aralkyloxy, aryloxy, OH, OSO3H, or SO3H). EXAMPLE:3-[ D(-)-alpha-( 4-Ethyl-2,3-dioxo-1-piperazinecarboxamido )-alpha-phenylacetamido]-4-trifluoromethyl-2-azetidinone-1-sulfonic acid. USE:Useful as a beta-lactam antibiotic or its intermediate. Showing a wide antibacterial spectrum against Gram-negative bacteria including Pseudomonas aeruginosa, and Gram-positive bacteria. PREPARATION:For example, a compound shown by the formula II is reacted with titanium dichloride in a mixed solvent of water and an alcohol or in an aqueous solution, to give an azatidinone derivative shown by the formula IIIamong the compound shown by the formula I. This compound is reacted with sulfuric anhydride to give a compound shown by the formula IV (M<+> is cation). |