Process for preparing 3-halogenated cephem derivative
    51.
    发明授权
    Process for preparing 3-halogenated cephem derivative 失效
    3-卤代头孢烯衍生物的制备方法

    公开(公告)号:US5919924A

    公开(公告)日:1999-07-06

    申请号:US849393

    申请日:1997-06-03

    CPC分类号: C07D501/00 Y02P20/55

    摘要: A process for preparing a 3-halogenated cephem derivative represented by the formula (2), characterized by causing a halogenating reagent to act on an allenyl .beta.-lactam compound represented by the formula (1) in the presence of a cuprous salt or cupric salt to obtain the 3-halogenated cephem derivative ##STR1## wherein R.sup.1 is a hydrogen atom, amino or protected amino, R.sup.2 is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl having at least one selected from hydroxyl and protected hydroxyl as a substituent, hydroxyl or protected hydroxyl, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, R.sup.4 is an aromatic compound residue which may have a substituent or nitrogen-containing aromatic heterocyclic compound residue which may have a substituent, and n is 0 to 2 ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, X is a halogen atom.

    摘要翻译: PCT No.PCT / JP96 / 03298 Sec。 371日期:1997年6月3日 102(e)日期1997年6月3日PCT 1996年11月8日PCT公布。 第WO97 / 17353号公报 日期:1997年5月5日制备式(2)表示的3-卤代头孢烯衍生物的方法,其特征在于,使卤化剂作用于由式(1)表示的丙烯酰基β-内酰胺化合物, 盐或铜盐,得到其中R 1为氢原子,氨基或被保护的氨基,R 2为氢原子,卤素原子,低级烷氧基,低级酰基,低级烷基,具有选自以下的至少一种的低级烷基的3-卤代头孢烯衍生物 羟基和保护的羟基作为取代基,羟基或被保护的羟基,R3是氢原子或羧酸保护基,R4是可以具有取代基的芳族化合物残基或可以具有取代基的含氮芳族杂环化合物残基,以及 n为0〜2,其中R1,R2和R3如上所定义,X为卤素原子。

    Process for preparation of 4-sulfonylthio azetidinone derivatives
    53.
    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

    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。

    Process for preparation of azetidinone derivatives
    54.
    发明授权
    Process for preparation of azetidinone derivatives 失效
    氮杂环丁酮衍生物的制备方法

    公开(公告)号:US4713452A

    公开(公告)日:1987-12-15

    申请号:US680723

    申请日:1984-12-12

    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 CN (VII)wherein R.sup.3 is 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R 3 SO 2 CN(Ⅶ)表示的化合物的芳族杂环残基,其中R 3如上定义。