| 摘要 |
<p>NEW MATERIAL:The azetidinone derivative of 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-dioxy-1-piperazinecarboxamido )-alpha-phenylacetamido]-4-trifluoromethyl-2-azetidinone-1-sulfonic acid tetrabutylammonium salt. USE:A derivative wherein R1 is acyl is useful as an antibiotic having broad antibacterial spectrum against Gram-negative and Gram-positive bacteria including Pseudomonas aeruginosa, and a derivative wherein R1 is H or amino-protecting group is expected to be useful as an intermediate of the above antibiotic. PREPARATION:The compound of formula I wherein R1 is amino-protecting group and X is H can be produced by reacting the compound of formula II with titanium trichloride in a mixture of water and alcohol or in an aqueous solution at 0-30 deg.C for 1-2hr.</p> |
