Process for the preparation of cephem compounds
    2.
    发明授权
    Process for the preparation of cephem compounds 有权
    头孢烯化合物的制备方法

    公开(公告)号:US06576761B1

    公开(公告)日:2003-06-10

    申请号:US10049048

    申请日:2002-02-07

    IPC分类号: C07D50122

    CPC分类号: C07D501/00 Y02P20/55

    摘要: 1. A process for preparing a 3-alkenylcephem compound or 3-norcephem compound of the formula (3) characterized in that an alkenyl halide of the formula (2), a nickel catalyst, a metal up to −0.3 (V/SCE) in standard oxidation reduction potential and a compound of a metal having a higher standard oxidation reduction potential than the metal are caused to act on a 3-cephem compound of the formula (1) in a solvent wherein R1 is a hydrogen atom or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or carboxylic acid protective group, and X is a halogen atom or the like, R4—Y  (2) wherein R4 is 1-alkenyl having or not having a substituent, and Y is a halogen atom wherein R1, R2 and R3 are as defined above, and R5 is a hydrogen atom or 1-alkenyl having or not having a substituent.

    摘要翻译: 1.一种制备式(3)的3-链烯基头孢烯化合物或3-诺卡波姆化合物的方法,其特征在于式(2)的烯基卤,镍催化剂,高达-0.3(V / SCE) 在标准氧化还原电位和具有比金属更高的标准氧化还原电位的金属的化合物在R1是氢原子等的溶剂中作用于式(1)的3-头孢烯化合物时,R2 是氢原子等,R 3为氢原子或羧酸保护基,X为卤素原子等,其中,R 4为具有或不具有取代基的1-烯基,Y为卤素原子,R1, R2和R3如上定义,R5是氢原子或具有或不具有取代基的1-烯基。

    Process for producing 3-alkenylcephem compounds
    3.
    发明授权
    Process for producing 3-alkenylcephem compounds 失效
    3-链烯基化合物的制备方法

    公开(公告)号:US06417351B1

    公开(公告)日:2002-07-09

    申请号:US09424260

    申请日:1999-12-01

    申请人: Yutaka Kameyama

    发明人: Yutaka Kameyama

    IPC分类号: C07D50122

    CPC分类号: C07D501/00 Y02P20/55

    摘要: A process for preparing 3-alkenylcephem compounds characterized in that 3-alkenylcephem compound of the formula (3) is prepared in a single step by simultaneously conducting reactions of a 3-chloromethylcephem compound of the formula (1) with iodization reagent, alkali metal hydroxide or carbonate, arylphosphine and an aldehyde of the formula (2)  R4—CHO  (2) wherein R1, R2, R3 and R4 are as defined in the specification.

    摘要翻译: 一种制备3-链烯基头孢烯化合物的方法,其特征在于通过同时进行式(1)的3-氯甲基头孢烯化合物与碘化试剂,碱金属氢氧化物的反应,在一个步骤中制备式(3)的3-链烯基头孢烯化合物 或碳酸酯,芳基膦和式(2)的醛,其中R 1,R 2,R 3和R 4如说明书中所定义。

    Process for the production of 3-vinyl cephalosporins
    4.
    发明授权
    Process for the production of 3-vinyl cephalosporins 失效
    生产3-乙烯基头孢菌素的方法

    公开(公告)号:US06414140B2

    公开(公告)日:2002-07-02

    申请号:US09792800

    申请日:2001-02-23

    IPC分类号: C07D50122

    CPC分类号: C07D501/00

    摘要: A process for the production of a 3-vinylcephalosporin compound of formula I wherein R1 and R2 denote hydrogen or an organic group by a Wittig reaction reacting first a compound of formula II with a compound of formula P(R4)3 or P(OR4)3 to produce a compound of formula III and secondly reacting the compound of formula III with a weak base of formula or of formula R10—COO−W+ wherein R5 is hydrogen, alkly or aryl and R6 and R7 are each an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2; or R5 and R8 are each aryl and R7 is an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2, W+ is an alkali metal cation and R10 is alkyl or aryl to produce a compound of formula IV and finally reacting a compound of formula IV with a compound of formula V to produce a compound of formula I.

    摘要翻译: 制备式I的3-乙酰头孢菌素化合物的方法,其中R1和R2通过维蒂希反应表示氢或有机基团,首先将式II化合物与式P(R4)3或P(OR4)3的化合物反应至 制备式III化合物,其次使式III化合物与式R 10 -COO-W +的弱碱反应,其中R 5是氢,烷基或芳基,R 6和R 7各自是式-COOR 8,-CN的活化基团 ,-SO 2 R 8,-COR 8或-CON(R 8)2; 或R 5和R 8各自为芳基,R 7为式-COOR 8,-CN,-SO 2 R 8,-COR 8或-CON(R 8)2的活化基团,W +为碱金属阳离子,R 10为烷基或芳基, 然后最终使式Ⅳ化合物与式Ⅴ化合物反应,生成式Ⅰ化合物。

    Intermediates for and synthesis of 3-methylene cephams
    5.
    发明授权
    Intermediates for and synthesis of 3-methylene cephams 失效
    3-亚甲基cephams的中间体和合成

    公开(公告)号:US06683176B2

    公开(公告)日:2004-01-27

    申请号:US09958857

    申请日:2001-12-31

    IPC分类号: C07D50122

    摘要: The present invention relates to novel processes for the preparation of 3-methylenecephams. More specifically, the present invention relates to the intramolecular cyclization of penicillin sulfoxide derived monocyclic azetidinone derivatives with organometallic catalysts of the formula III. MEx(H2O)y  (III) wherein: M is Sc, Y, La, Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Zr, Hf, Th, Nb, Ta, U, Bi, or In; E is O[SO2(C1-C6 polyfluoroalkyl)], N[SO2(C1-C6 polyfluoroalkyl)]2, or C[SO2(C1-C6 polyfluoroalkyl)]3; x is 3; y is 0, 1, 2, 3, 4, 5, 6, 7, 8, or 9.

    摘要翻译: 本发明涉及制备3-亚甲基脑炎的新方法。 更具体地说,本发明涉及由式III的有机金属催化剂衍生的青霉素亚砜衍生的单环氮杂环丁酮衍生物的分子内环化,其中M为Sc,Y,La,Ce,Pr,Nd,Sm,Eu,Gd,Tb, Dy,Ho,Er,Tm,Yb,Lu,Zr,Hf,Th,Nb,Ta,U,Bi或In; E是O [SO2(C1-C6多氟烷基)],N [SO2(C1-C6多氟烷基 )] 2或C [SO 2(C 1 -C 6多氟烷基)] 3; x为3; y为0,1,2,3,4,5,6,7,8或9。

    Purification process
    7.
    发明授权
    Purification process 失效
    净化过程

    公开(公告)号:US06835829B2

    公开(公告)日:2004-12-28

    申请号:US10348569

    申请日:2003-01-21

    IPC分类号: C07D50122

    CPC分类号: C07D501/00

    摘要: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.

    摘要翻译: 乙烯基ACA与7-ADCA的混合物中通过乙烯基-ACA或通过色谱法的新型盐消耗7-ADCA的方法。