Cephalosporin vinyl halides
    51.
    发明授权
    Cephalosporin vinyl halides 失效
    头孢菌素乙烯基卤化物

    公开(公告)号:US4299954A

    公开(公告)日:1981-11-10

    申请号:US091603

    申请日:1979-11-05

    申请人: Douglas O. Spry

    发明人: Douglas O. Spry

    IPC分类号: C07D501/20

    摘要: 7-Acylamino-2-halomethylidene-3-methyl and 3-acetoxymethyl-3-cephem-4-carboxylic acids and esters are prepared via reaction of the corresponding 2-exomethylene-3-cephem ester sulfoxides with chloro (or bromo) dimethyliminium chlorides (or bromides). The 2-halomethylidene derivatives are useful as antimicrobial agents and intermediates to novel 2-acyloxymethylidene cephalosporins and to the known 2-aryl (or alkyl) mercaptomethylidene cephalosporins.

    摘要翻译: 7-酰基氨基-2-卤代亚甲基-3-甲基和3-乙酰氧基甲基-3-头孢烯-4-羧酸和酯通过相应的2-异亚甲基-3-头孢烯酯亚砜与氯(或溴)二甲基亚胺鎓氯化物 (或溴化物)。 2-卤代亚甲基衍生物可用作新型2-酰氧基亚甲基头孢菌素和已知的2-芳基(或烷基)巯基亚甲基头孢菌素的抗微生物剂和中间体。

    7.beta.-Hydroxy-3-heterocyclicthio-methyl cephalosporin intermediates
    53.
    发明授权
    7.beta.-Hydroxy-3-heterocyclicthio-methyl cephalosporin intermediates 失效
    7β-羟基-3-杂环硫代甲基头孢菌素中间体

    公开(公告)号:US4218564A

    公开(公告)日:1980-08-19

    申请号:US746356

    申请日:1976-12-01

    申请人: John G. Gleason

    发明人: John G. Gleason

    IPC分类号: C07D501/00

    CPC分类号: C07D501/04 C07D501/00

    摘要: The compounds of this invention are 7.beta.-hydroxy-3-heterocyclicthiomethyl cephalosporins useful as intermediates for the preparation of 7.beta.-acyloxy cephalosporins.

    摘要翻译: 本发明的化合物是用作制备7β-酰氧基头孢菌素的中间体的7β-羟基-3-杂环硫代甲基头孢菌素。

    Cephalosporins having a metaloxy group in 3-substituent
    56.
    发明授权
    Cephalosporins having a metaloxy group in 3-substituent 失效
    在3-取代基中具有金属氧基的头孢菌素

    公开(公告)号:US4092474A

    公开(公告)日:1978-05-30

    申请号:US637477

    申请日:1975-12-03

    摘要: Antibacterial cephalosporins of the formula ##STR1## wherein Acyl is an acyl group; R is a hydrogen or methoxy, R.sup.1 is a hydrocarbyl group containing 1 to 8 carbon atoms; R.sup.2 is a hydrogen, alkali metal, alkaline earth metal, halo-alkaline earth metal group or acyl group containing 1 to 12 carbon atoms; R.sup.3 is a hydrogen, pharmaceutically acceptable cation, or ester residue; or when R.sup.2 and R.sup.3 are both hydrogens, they can be combined to form a lactone ring; the broken line shows a double bond at position 2 or 3; and n is zero or one, and processes for preparing them by the reaction of the compound shown by above formula in which R.sup.1 and R.sup.2 combined to show a bond, with a Grignard type or organometallic reagent to introduce R.sup.1, followed by acylation, oxidation, reduction, double bond migration, or other reactions.

    摘要翻译: 其中酰基是酰基的式“IMAGE”的抗菌头孢菌素; R是氢或甲氧基,R 1是含有1至8个碳原子的烃基; R2是含有1〜12个碳原子的氢,碱金属,碱土金属,卤代 - 碱土金属或酰基; R3是氢,药学上可接受的阳离子或酯残基; 或当R 2和R 3均为氢时,它们可以组合形成内酯环; 虚线显示位置2或3的双键; 并且n为0或1,并且通过上式所示的化合物(其中R 1和R 2结合表示键)与格利雅类型或有机金属试剂反应以制备它们的方法以引入R1,然后酰化,氧化, 还原,双键迁移或其他反应。

    Methods of combatting bacterial infections in warm-blooded animal with
cephalsporin R-sulfoxide
    57.
    发明授权
    Methods of combatting bacterial infections in warm-blooded animal with cephalsporin R-sulfoxide 失效
    使用辣椒素R-亚砜处理温血动物细菌感染的方法

    公开(公告)号:US4075337A

    公开(公告)日:1978-02-21

    申请号:US633006

    申请日:1975-11-18

    摘要: R-sulfoxides of the formulae ##STR1## wherein ##STR2## represents an usual penicillin or cephalosporin amide group and X is selected from the group consisting of hydrogen, hydroxy, an alkanoyloxy and the residue of a nucleophilic agent and their salts and esters are prepared by oxidation of the corresponding penicillins and cephalosporins to convert the sulfur atom in the ring to a sulfoxide group and separating and isolating the penicillin- or cephalosporin R-sulfoxide so formed from the reaction mixture or by acylation of the free amino group of the intermediate 6-aminopenicillanic acid R-sulfoxide and 7-aminocephalosporanic acid R-sulfoxide and derivatives. A preferred straight oxidation method is the photosensitized oxygenation method.

    摘要翻译: 其中代表通常的青霉素或头孢菌素酰胺基团,X选自氢,羟基,烷酰氧基和亲核残基的R-亚砜 通过氧化相应的青霉素和头孢菌素以将环中的硫原子转化成亚砜基团并分离和分离由反应混合物形成的青霉素或头孢菌素R-亚砜,或通过酰化 中间体6-氨基青霉烷酸R-亚砜的游离氨基和7-氨基头孢烷酸R-亚砜及其衍生物。 优选的直接氧化法是光敏氧合法。

    Process for the preparation of cephalosporin antibiotics
    58.
    发明授权
    Process for the preparation of cephalosporin antibiotics 失效
    制备西酞普兰抗生素的方法

    公开(公告)号:US4053286A

    公开(公告)日:1977-10-11

    申请号:US689408

    申请日:1976-05-24

    IPC分类号: C07D501/04 C07D501/06

    CPC分类号: C07D501/04 C07D501/06

    摘要: An improved process for preparing the compound 7.beta.-(2-thienylacetamido)-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-carboxylic acid or its esters, from the compound 7.beta.-(D-5-amino-5-carboxyvaleramido)-3-carbamoyloxymethyl-7-methoxy-3-cephem-4-carboxylic acid, by conducting the transacylation of the latter compound in the presence of commercially available alumino-silicate zeolites, also known as "molecular sieves." The process can be employed to prepare a cephalosporin with a desired 7-acylamido group from cephalosporins having a broad range of different 7-acylamido groups without having to isolate and purify a 7-amino intermediate. The final products have utility as broad spectrum antibiotics.

    4-Thio substituted-.DELTA..sup.2 -cephalosporin intermediates
    60.
    发明授权
    4-Thio substituted-.DELTA..sup.2 -cephalosporin intermediates 失效
    4-硫代替代 - {66 {hu 2 {b-头孢菌素中间体

    公开(公告)号:US4039534A

    公开(公告)日:1977-08-02

    申请号:US632618

    申请日:1975-11-17

    CPC分类号: C07D501/04 C07D501/60

    摘要: Cephalosporin intermediates of the formulas ##STR1## wherein R is lower alkyl, 2,2,2-trichloroethyl, diphenylmethyl, p-methoxybenzyl, or p-nitrobenzyl; R.sub.1 is lower alkyl or phenyl; R.sub.2 is hydrogen or acetoxy; R.sub.4 is methyl or ethyl; and R.sub.5 is hydrogen, methyl, or methoxy; are disclosed. Methods of reacting these intermediates to prepare antibacterially active cephalosporins are disclosed.

    摘要翻译: 其中R为低级烷基,2,2,2-三氯乙基,二苯基甲基,对甲氧基苄基或对硝基苄基的式“IMAGE”和“IMAGE”的头孢菌素中间体; R1是低级烷基或苯基; R2是氢或乙酰氧基; R4是甲基或乙基; 和R5是氢,甲基或甲氧基; 被披露。 公开了使这些中间体反应制备抗菌活性头孢菌素的方法。