Process for preparing thiazolino azetidinone and 2-exo-methylenepenam
derivative
    2.
    发明授权
    Process for preparing thiazolino azetidinone and 2-exo-methylenepenam derivative 失效
    制备噻唑基氮杂环丁酮和2-外 - 亚甲基台am am嗪衍生物的方法

    公开(公告)号:US5288860A

    公开(公告)日:1994-02-22

    申请号:US3024

    申请日:1993-01-11

    摘要: The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.

    摘要翻译: 本发明提供由式(1)表示的噻唑并氮杂环丁酮衍生物,其中R 1是具有或不具有取代基的苯基,具有或不具有取代基的甲基或基团,R3是具有或不具有取代基的苯基, 不具有取代基,R2为氢原子或羧酸保护基,及其制备方法。 本发明进一步提供了制备2-异亚甲基台内叶酸衍生物的方法,其特征在于水解上述式(1)的噻唑并氮杂环丁酮衍生物的噻唑啉环以进行再循环,得到式(1)所示的2-外 - 亚甲基山梨醇衍生物, 图像(3)其中R1和R2如上所定义。

    Process for preparing 3-alkoxymethylcephem compounds
    5.
    发明授权
    Process for preparing 3-alkoxymethylcephem compounds 失效
    制备3-烷氧基甲基头孢烯化合物的方法

    公开(公告)号:US5968335A

    公开(公告)日:1999-10-19

    申请号:US945850

    申请日:1997-11-07

    CPC分类号: C25B3/02

    摘要: A process for preparing a 3-alkoxymethylcephem compound represented by the formula (II) ##STR1## where R.sub.1 is a hydrogen atom, amino or protected amino, R.sub.3 is a hydrogen atom or carboxylic acid protective group and R.sub.4 is lower alkyl, which process is characterized in that a 3-thiomethylcephem compound represented by the formula (I) ##STR2## where R.sub.1 and R.sub.3 are as defined above and R.sub.2 is aryl which may have a substituent, is electrolytically oxidized in an electrooxidation reaction system in the presence of a lower alcohol using as a positive electrode, a material selected from the group consisting of platinum, tin, aluminum, stainless steel, nickel, lead oxide, carbon, iron oxide and titanium, to obtain the 3-alkoxymethylcephem compound.

    摘要翻译: PCT No.PCT / JP97 / 00708 Sec。 371日期:1997年11月7日 102(e)日期1997年11月7日PCT 1997年3月7日PCT公布。 出版物WO97 / 34027 日期:1997年9月18日制备式(II)表示的3-烷氧基甲基头孢烯化合物的方法,其中R1是氢原子,氨基或被保护的氨基,R3是氢原子或羧酸保护基,R4是低级烷基, 方法的特征在于,其中R 1和R 3如上所定义,R 2为可具有取代基的芳基的式(I)表示的3-硫代甲基头孢烯化合物在电氧化反应体系中在低级醇存在下被电解氧化 使用选自铂,锡,铝,不锈钢,镍,氧化铅,碳,氧化铁和钛的材料作为正极,得到3-烷氧基甲基头孢烯化合物。

    Process for preparing 3-halogenated cephem derivative
    6.
    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 preparing 2-isocephem derivatives
    7.
    发明授权
    Process for preparing 2-isocephem derivatives 失效
    制备2-异头孢烯衍生物的方法

    公开(公告)号:US5688942A

    公开(公告)日:1997-11-18

    申请号:US732446

    申请日:1996-11-06

    摘要: A process for preparing a 2-isocephem derivative characterized in that a thioacetic acid derivative which itself is basic or a mixture of a base and a thioacetic acid derivative is caused to act on a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by the general formula (1) in a water-containing organic solvent to obtain a 3-halomethyl-2-isocephem derivative represented by the general formula (2), and a process for preparing a 2-oxaisocephem derivative characterized in that a base is caused to act on a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by the general formula (1) in a water-containing organic solvent to obtain a 3-halomethyl-2-oxaisocephem derivative represented by the general formula (3) ##STR1## wherein R.sup.1 is a hydrogen atom, amino or protected amino, R.sup.2 is a hydrogen atom or lower alkoxyl, R.sup.1 and R.sup.2, when taken together, form a cyclic amino protecting group, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, W is a leaving group, and X and Y are the same or different and are each a halogen atom ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and X are the same as above, ##STR3## wherein R.sup.1, R.sup.2, R.sup.3 and X are the same as above.

    摘要翻译: PCT No.PCT / JP96 / 00538 Sec。 371日期:1996年11月6日 102(e)日期1996年11月6日PCT 1996年3月6日PCT公布。 公开号WO96 / 28453 日期1996年9月19日制备2-异头孢烯衍生物的方法,其特征在于使本身为碱性的硫代乙酸衍生物或碱和硫代乙酸衍生物的混合物作用于2-氮杂环丁烷基-3,4- 由通式(1)表示的二卤代-2-丁烯酸化合物在含水有机溶剂中得到由通式(2)表示的3-卤代甲基-2-异头孢烯衍生物,以及制备2- 恶唑磺酸衍生物,其特征在于使碱在含水有机溶剂中作用于由通式(1)表示的2-氮杂环丁烷基-3,4-二卤代-2-丁烯酸化合物,得到3-卤代甲基 - 由通式(3)表示的2-氧代硫代衍生物无或被保护的氨基,R2是氢原子或低级烷氧基,R1和R2一起形成环状氨基保护基,R3是氢原子或羧酸保护基 组,W是离职小组,X和Y是sam e或不同,各自为卤素原子,其中R1,R2,R3和X与上述相同,其中R1,R2,R3和X与上述相同。