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    • 3. 发明授权
    • Process for preparation of 4-sulfonylthio azetidinone derivatives
    • 4-磺酰硫基氮杂环丁酮衍生物的制备方法
    • US4740596A
    • 1988-04-26
    • US089947
    • 1987-08-26
    • Sigeru ToriiHideo TanakaMichio SasaokaShigemitsu Nagao
    • Sigeru ToriiHideo TanakaMichio SasaokaShigemitsu Nagao
    • C07D205/08A61K31/395A61K31/397A61P31/04C07D205/09C07D205/095C07D417/12C07B45/00C07D401/12
    • C07D205/09C07D205/095
    • A process for preparing an azetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is hydrogen, halogen or lower alkoxy, R.sup.2 is hydrogen, halogen, lower alkoxy, amino or a group ##STR2## (in which R.sup.5 is substituted or unsubstituted phenyl, substituted or unsubstituted phenylmethyl, substituted or unsubstituted phenoxymethyl, or substituted or unsubstituted benzoyl), or R.sup.1 and R.sup.2, when taken together, are carbonyl, R.sup.3 is substituted or unsubstituted phenyl, and R.sup.4 is hydrogen, optionally substituted hydrocarbon residue or acyl, silyl, sulfonyl or phosphonyl derived from inorganic acid or organic acid, the process comprising reacting a dithioazetidinone derivative represented by the formula ##STR3## wherein R.sup.1, R.sup.2 and R.sup.4 are as defined above and R.sup.9 is substituted or unsubstituted, nitrogen-containing aromatic heterocyclic residue with a compound represented by the formulaR.sup.3 SO.sub.2 SR.sup.9 (VII)wherein R.sup.3 and R.sup.9 are as defined above.
    • 制备式(I)表示的氮杂环丁酮衍生物的方法,其中R 1是氢,卤素或低级烷氧基,R 2是氢,卤素,低级烷氧基,氨基或基团(其中R 5是取代的或 未取代的苯基,取代或未取代的苯基甲基,取代或未取代的苯氧基甲基或取代或未取代的苯甲酰基),或R 1和R 2一起为羰基,R 3为取代或未取代的苯基,且R 4为氢,任选取代的烃残基或酰基 ,衍生自无机酸或有机酸的甲硅烷基,磺酰基或膦酰基,该方法包括使由式(VI)表示的二硫代氮杂环丁酮衍生物(其中R 1,R 2和R 4如上所定义)和R 9是取代或未取代的, 含有由式R3SO2SR9(VII)表示的化合物的芳族杂环残基,其中R3和R9如上定义。