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    Process for preparation of 4-sulfonylthio azetidinone derivatives
    3.
    发明授权
    Process for preparation of 4-sulfonylthio azetidinone derivatives 失效
    4-磺酰硫基氮杂环丁酮衍生物的制备方法

    公开(公告)号：US4740596A

    公开(公告)日：1988-04-26

    申请号：US089947

    申请日：1987-08-26

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Michio Sasaoka ,  Shigemitsu Nagao

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Michio Sasaoka ,  Shigemitsu Nagao

    IPC分类号： C07D205/08 ,  A61K31/395 ,  A61K31/397 ,  A61P31/04 ,  C07D205/09 ,  C07D205/095 ,  C07D417/12 ,  C07B45/00 ,  C07D401/12

    CPC分类号： C07D205/09 ,  C07D205/095

    摘要： 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.

    摘要翻译： 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。

    Azetidinone disulfides and a ring opening process for preparing the same
    6.
    发明授权
    Azetidinone disulfides and a ring opening process for preparing the same 失效
    氮杂环丁酮二硫化物及其制备方法

    公开(公告)号：US4801720A

    公开(公告)日：1989-01-31

    申请号：US46444

    申请日：1987-05-06

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Siroi

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Junzo Nokami ,  Michio Sasaoka ,  Norio Saito ,  Takashi Siroi

    IPC分类号： C07D205/08 ,  C07D205/095 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14 ,  C07D501/20 ,  C07D501/36 ,  C07B43/06 ,  C07B45/00 ,  C07D401/12

    CPC分类号： C07D403/12 ,  C07D205/095 ,  C07D417/12 ,  C07D417/14 ,  Y02P20/55

    摘要： An azetidinone derivative represented by the formula (I) ##STR1## wherein R.sup.1 is substituted or unsubstituted phenyl or substituted or unsubstituted phenoxy, R.sup.2 is hydrogen, optionally substituted hydrocarbon residue or amino-protecting group selected from acyl, silyl, sulfonyl and phosphonyl derived from organic or inorganic acid, ##STR2## is >C.dbd.O or>C.dbd.N--OR.sup.3 (wherein R.sup.3 is hydrogen or lower alkyl), X.sup.1 and X.sup.2 are the same or different and are halogen, hydroxyl, alkoxy, acyloxy, SR.sup.4 (wherein R.sup.4 is straight chain or branched chain lower alkyl substituted or unsubstituted, substituted or unsubstituted phenyl or substituted or unsubstituted heterocyclic group), amino or hydrogen, one of X.sup.1 and X.sup.2 being hydrogen when the other is not, and R.sup.5 is substituted or unsubstituted phenyl or substituted or unsubstituted heterocyclic group, and a process for preparing the same.

    摘要翻译： 由式（I）表示的氮杂环丁酮衍生物其中R1是取代或未取代的苯基或取代或未取代的苯氧基，R2是氢，任选取代的烃残基或氨基保护基，其选自酰基，甲硅烷基，磺酰基和 衍生自有机或无机酸的膦酰基是C = O或C = N-OR 3（其中R 3为氢或低级烷基），X 1和X 2相同或不同，为卤素，羟基，烷氧基，酰氧基 ，SR4（其中R4是直链或支链低级烷基取代或未取代的，取代或未取代的苯基或取代或未取代的杂环基），氨基或氢，当另一个未被取代时，X 1和X 2之一为氢，R 5为取代基 或未取代的苯基或取代或未取代的杂环基，及其制备方法。

    Process for preparing azetidinone derivatives
    8.
    发明授权
    Process for preparing azetidinone derivatives 失效
    制备氮杂环丁酮衍生物的方法

    公开(公告)号：US4566996A

    公开(公告)日：1986-01-28

    申请号：US567736

    申请日：1984-01-03

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Takashi Shiroi ,  Michio Sasaoka ,  Norio Saito ,  Kiyotoshi Matsumura

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Takashi Shiroi ,  Michio Sasaoka ,  Norio Saito ,  Kiyotoshi Matsumura

    IPC分类号： C07D205/08 ,  C07D205/095 ,  C07D405/12

    CPC分类号： C07D205/095 ,  Y02P20/55

    摘要： A process for preparing an azetidinone derivative represented by the formula (1) ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aryl group, a substituted or unsubstituted phenylmethyl group or a substituted or unsubstituted phenoxymethyl group, R.sup.2 represents a hydrogen atom or a group for protecting carboxylic acid and Ar represents a substituted or unsubstituted phenyl group, the process comprising reacting a thiazolineazetidinone derivative represented by the formula (2) ##STR2## wherein R.sup.1 and R.sup.2 are as defined above with a sulfonyl bromide represented by the formula (3)Ar--SO.sub.2 --Br (3)wherein Ar is as defined above in water-containing organic solvent.

    摘要翻译： 制备由式（1）表示的氮杂环丁酮衍生物的方法其中R1表示取代或未取代的芳基，取代或未取代的苯基甲基或取代或未取代的苯氧基甲基，R2表示氢原子或 用于保护羧酸和Ar的基团代表取代或未取代的苯基，该方法包括使式（2）表示的噻唑啉氮杂环丁酮衍生物（2）其中R1和R2如上定义， 式（3）Ar-SO 2-Br（3）其中Ar如上所述在含水有机溶剂中。