Method for production of 3-exomethylenecepham derivatives
    1.
    发明公开
    Method for production of 3-exomethylenecepham derivatives 失效
    Verfahren zur Herstellung von 3-Exomethylencepham-Derivaten。

    公开(公告)号:EP0341694A2

    公开(公告)日:1989-11-15

    申请号:EP89108427.9

    申请日:1989-05-10

    IPC分类号: C07D501/04

    CPC分类号: C07D501/04 Y02P20/55

    摘要: Disclosed is a method of producing a 3-exo­methylenecepham of the formula
    wherein R¹ is amino or substituted amino and R² is a carboxyl-protecting group comprising reacting a cephem of the formula
    wherein R¹ and R² are as defined above and X is halogen with lead metal while maintaining the pH of the reac­tion system at about 0.1 to 8. The cephem (I) may be reacted with a catalytic amount of lead metal or a lead compound in the presence of a metal having a greater ionization tendency than lead.

    摘要翻译: 公开了一种制备式CHEM的3-异亚甲基脑炎的方法,其中R 1是氨基或取代的氨基,R 2是羧基保护基,其包括使式CHEM的头孢烯反应, 1>和R 2如上所定义,X是卤素与铅金属,同时将反应体系的pH保持在约0.1至8℃。头孢烯(I)可以与催化量的铅金属或铅 在具有比铅更大的电离倾向的金属的存在下进行化合物。

    Process for preparation of beta-lactam derivatives
    2.
    发明公开
    Process for preparation of beta-lactam derivatives 失效
    制备BETA-LACTAM衍生物的方法

    公开(公告)号:EP0444708A3

    公开(公告)日:1992-06-10

    申请号:EP91103135.9

    申请日:1991-03-01

    摘要: The invention provides a process for preparing a β-lactam derivative represented by the following formula (2) and/or the corresponding enol tautomer (which may be produced depending on its structure), the process comprising oxidizing an alkenyl-substituted β-lactam derivative represented by the following formula (1) in the presence of a ruthenium catalyst or a rhenium catalyst using a periodic acid or a salt thereof:

    wherein R¹ is a hydrogen atom, a C₁₋₄ alkyl group or a C₁₋₄ haloakyl group, R² is a hydrogen atom, a C₁₋₄ alkyl group or a phenyl group which may have a substituent, A is a group represented by the formula

    a group represented by the formula

    or a group represented by the formula

    wherein R³ is an amino group or a protected amino group, R⁴ is a hydrogen atom or a group for protecting a carboxylic acid, one of R⁵ and R⁶ is a hydrogen atom and the other is either a hydroxyl group or a protected hydroxyl group, or R⁵ and R⁶, when taken together, represent an oxo group or a group represented by the formula

    wherein R⁷ is a hydrogen atom, a C₁₋₄ alkyl group, a phenyl group which may have a substituent, or a group -COOR⁸ wherein R⁸ is a hydrogen atom or a C₁₋₄ alkyl group, X is a hydrogen atom, a halogen atom, a hydroxyl group or a protected hydroxyl group, and Y is a group of the formula -SO₂Ar or -SAr wherein Ar is an aryl group which may have a substituent or a nitrogen-containing aromatic heterocyclic group which may have a substituent; and

    wherein R¹ and A are as defined above.

    Method of Preparing a Halogenated Compound
    4.
    发明公开
    Method of Preparing a Halogenated Compound 有权
    Verfahren zur Herstellung von einer haloierten Verbindung

    公开(公告)号:EP1319642A2

    公开(公告)日:2003-06-18

    申请号:EP03003782.4

    申请日:1998-12-10

    IPC分类号: C07B39/00 C07C257/02

    摘要: A halogenated compound of formula A-X is prepared by reacting in an organic solvent at least one halogenatihg agent selected from halogenating agents of formula
    and halogenating agents of formula
    and at least one compound selected from lower alkyl sulfones, lower alkenyl sulfones, aryl sulfones and heterocyclic sulfones at the same time,
    with a hydroxyl group containing compound of the formula A - OH.

    摘要翻译: 式AX的卤代化合物通过在有机溶剂中使至少一种选自式CHEM的卤化剂和式CHEM的卤化剂的卤化剂与至少一种选自低级烷基砜,低级烯基砜的化合物 芳基砜和杂环砜同时与含羟基的式A-OH化合物反应。

    Process for preparation of beta-lactam derivatives
    5.
    发明公开
    Process for preparation of beta-lactam derivatives 失效
    Verfahren zur Herstellung von beta-Lactamderivaten。

    公开(公告)号:EP0444708A2

    公开(公告)日:1991-09-04

    申请号:EP91103135.9

    申请日:1991-03-01

    摘要: The invention provides a process for preparing a β-lactam derivative represented by the following formula (2) and/or the corresponding enol tautomer (which may be produced depending on its structure), the process comprising oxidizing an alkenyl-substituted β-lactam derivative represented by the following formula (1) in the presence of a ruthenium catalyst or a rhenium catalyst using a periodic acid or a salt thereof:

    wherein R¹ is a hydrogen atom, a C₁₋₄ alkyl group or a C₁₋₄ haloakyl group, R² is a hydrogen atom, a C₁₋₄ alkyl group or a phenyl group which may have a substituent, A is a group represented by the formula

    a group represented by the formula

    or a group represented by the formula

    wherein R³ is an amino group or a protected amino group, R⁴ is a hydrogen atom or a group for protecting a carboxylic acid, one of R⁵ and R⁶ is a hydrogen atom and the other is either a hydroxyl group or a protected hydroxyl group, or R⁵ and R⁶, when taken together, represent an oxo group or a group represented by the formula

    wherein R⁷ is a hydrogen atom, a C₁₋₄ alkyl group, a phenyl group which may have a substituent, or a group -COOR⁸ wherein R⁸ is a hydrogen atom or a C₁₋₄ alkyl group, X is a hydrogen atom, a halogen atom, a hydroxyl group or a protected hydroxyl group, and Y is a group of the formula -SO₂Ar or -SAr wherein Ar is an aryl group which may have a substituent or a nitrogen-containing aromatic heterocyclic group which may have a substituent; and

    wherein R¹ and A are as defined above.

    摘要翻译: 本发明提供了制备由下式(2)表示的β-内酰胺衍生物和/或相应的烯醇互变异构体(其可根据其结构产生)的方法,该方法包括将烯基取代的β-内酰胺衍生物 在钌催化剂或使用高碘酸或其盐的铼催化剂存在下,由下式(1)表示:其中R 1是氢原子,C 1-4烷基或C 1 -4卤代烷基,R 2是氢原子,可以具有取代基的C 1-4烷基或苯基,A是下式表示的基团:CHEM>由式CHEM> 或由式表示的基团,其中R 3是氨基或被保护的氨基,R 4是氢原子或用于保护羧酸的基团,R 5和R 5之一 <6>是氢原子,另一个是羟基或被保护的羟基,或R 5和R 6, 一起代表一个氧代基团或由式表示的基团,其中R 7是氢原子,C 1-4烷基,可以具有取代基的苯基或-COOR基团, 其中R 8是氢原子或C 1-4烷基,X是氢原子,卤素原子,羟基或保护的羟基,Y是式-SO 2 Ar或 - SAr其中Ar是可以具有取代基的芳基或可以具有取代基的含氮芳族杂环基; 和,其中R 1和A如上所定义。 Ø