申请人:Otsuka Kagaku Kabushiki Kaisha
公开号:US04740596A1
公开(公告)日:1988-04-26
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 formula R.sup.3 SO.sub.2 SR.sup.9 (VII) wherein R.sup.3 and R.sup.9 are as defined above.
一种制备式为##STR1##的氮杂环丙酮衍生物的方法,其中R.sup.1为氢、卤素或低烷氧基,R.sup.2为氢、卤素、低烷氧基、氨基或者一个基团##STR2##(其中R.sup.5为取代或未取代的苯基、取代或未取代的苯甲基、取代或未取代的苯氧甲基或取代或未取代的苯甲酰基),或者当R.sup.1和R.sup.2在一起时,它们是羰基,R.sup.3为取代或未取代的苯基,R.sup.4为氢、可选的取代烃基残基或来自无机酸或有机酸的酰基、硅基、磺酰基或膦酸基衍生物,所述方法包括将式为##STR3##的二硫代氮杂环丙酮衍生物与式为R.sup.3 SO.sub.2 SR.sup.9(VII)的化合物反应,其中R.sup.3和R.sup.9如上所定义,R.sup.9为取代或未取代的含氮芳香杂环残基。