| 摘要 |
<p>NEW MATERIAL:a compound expressed by formula I [R<1> is lower alkyl, lower alkenyl, cycloalkyl or aryl; R<2> is H, lower alkyl or (lower alkyl)amino, etc.; R<3> is H, lower alkyl, lower alkoxy or halogen, etc.; X is halogen]. EXAMPLE:7-(1-benzyloxycarbonylaminocyclopropyl)-9-cyclopropyl-6,8- difluoro-2,3,4,9-tetrahydroisothiazolo[5,4-b]quinoline-3,4-dione. USE:Having strong anti-fungus activity against antibiotic resistant fungus. PREPARATION:A compound expressed by formula II (R<5> is H or carboxyl protecting group) is used as raw material to obtain a compound expressed by formula III and the compound expressed by formula III is reacted with hydroxylamine-O-sulfonate in a solvent such as water-containing tetrahydrofuran in the presence of base (e.g. sodium bicarbonate).</p> |
