3-Thiovinyl-cephalosporins
    31.
    发明授权
    3-Thiovinyl-cephalosporins 失效
    3-硫代乙烯基头孢菌素

    公开(公告)号:US4307116A

    公开(公告)日:1981-12-22

    申请号:US152115

    申请日:1980-05-21

    CPC分类号: C07D501/24

    摘要: Novel cephalosporins of the general formula (I); ##STR1## in which R is alkyl, L-2-amino-2-carboxy-ethyl, phenyl, pyridyl, pyridyl-N-oxide, pyrimidin-2-yl, substituted pyridazin-3-yl, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 4-position, 1,3,4-triazol-5-yl or 2-alkoxycarbonyl-1,3,4-triazol-5-yl substituted in the 1-position, 1,4-dialkyl-5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl, 1-alkyl-5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl, 2-alkyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl, triazol-5-yl, 1,3,4-thiadiazol-5-yl which is substituted or unsubstituted, 1,2,4-thiadiazol-5-yl which is substituted, 1,3,4-oxadiazol-5-yl which is substituted or unsubstituted, oxazol-2-yl which is substituted or unsubstituted or tetrazol-5-yl which is substituted or unsubstituted in the 1-position, R' is a hydrogen atom or a radical of the general formula (II); ##STR2## and R.sup.o is hydrogen, alkyl, vinyl or cyanomethyl, as well as their salts, are useful as anti-bacterial agents.

    摘要翻译: 通式(I)的新型头孢菌素; (I)其中R是烷基,L-2-氨基-2-羧基 - 乙基,苯基,吡啶基,吡啶基-N-氧化物,嘧啶-2-基,取代的哒嗪-3-基,5,6 在4-位取代的1-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基,1,3,4-三唑-5-基或2-烷氧基羰基-1,3 在1-位上取代的4-三唑-5-基,1,4-二烷基-5,6-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基,1 - 烷基-5,6-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基,2-烷基-5,6-二氧代-1,2,5,6-四氢 -1,2,4-三嗪-3-基,三唑-5-基,取代或未取代的1,3,4-噻二唑-5-基,被取代的1,2,4-噻二唑-5-基 被取代或未取代的取代或未取代的1,3,4-恶二唑-5-基,在1位被取代或未取代的四唑-5-基,R'是氢 原子或通式(II)的基团; (II)和Ro是氢,烷基,乙烯基或氰基甲基,以及它们的盐可用作抗细菌剂。

    Thioloesters
    34.
    发明授权
    Thioloesters 失效
    硫铁矿

    公开(公告)号:US4385181A

    公开(公告)日:1983-05-24

    申请号:US233109

    申请日:1981-02-10

    CPC分类号: C07D253/075 C07D501/24

    摘要: New thioloesters of the formula: ##STR1## wherein R.degree. represents hydrogen, alkyl, vinyl, cyanomethyl or a protecting radical, R' represents hydrogen or a protecting radical, R represents alkyl, L-2-amino-2-carboxyethyl, phenyl or various heterocyclic radicals, and their syn and anti isomers and mixtures thereof, and metal salts thereof and addition salts thereof with tertiary nitrogen-containing bases, are intermediates useful in the preparation of cephalosporins having anti-bacterial properties.

    摘要翻译: 新的硫代酯,其结构式如下:其中R DEG表示氢,烷基,乙烯基,氰基甲基或保护基,R'表示氢或保护基,R表示烷基,L-2-氨基-2-羧乙基,苯基或 各种杂环基以及它们的顺式和反式异构体及其混合物及其金属盐及其与叔氮基的加成盐是可用于制备具有抗细菌特性的头孢菌素的中间体。

    3-Vinyl-cephalosporins
    36.
    发明授权
    3-Vinyl-cephalosporins 失效
    3-乙烯基 - 头孢菌素

    公开(公告)号:US4307230A

    公开(公告)日:1981-12-22

    申请号:US152084

    申请日:1980-05-21

    摘要: Novel 3-vinyl-cephalosporins of the formula ##STR1## in which n is 0 or 1, R.sub.1 is hydrogen, a radical of the formula ##STR2## [in which R.sub.4 is hydrogen or a protective radical and R.sub.5 is hydrogen, alkyl, vinyl or cyanomethyl or is a protective radical], or a protective radical, and R.sub.2 is hydrogen, a protective radical or an enzymatically removable radical, or R.sub.1 is hydrogen or an acyl radical which may carry various substituents and R.sub.2 is hydrogen or a protective radical, and R.sub.3 is a radical of the general formula R'.sub.3 --SO.sub.2 --O-- or R".sub.3 --CO--O--, in which R'.sub.3 is alkyl, trifluoromethyl, trichloromethyl or phenyl which is substituted by a halogen atom or by an alkyl or nitro radical, and R".sub.3 is defined like R'.sub.3 or represents methyl which is substituted by acyl or alkoxycarbonyl, or represents ethyl or propyl substituted in the 2-position by acyl or alkoxycarbonyl. These compounds are useful as intermediates for the preparation of antibiotic 3-thiovinyl-cephalosporins.

    摘要翻译: 式(I)的新型3-乙烯基头孢菌素其中n为0或1,R 1为氢,式(II)的基团[其中R 4为氢或保护基,R 5为 是氢,烷基,乙烯基或氰基甲基,或是保护基]或保护基,R2是氢,保护基或酶可除去的基团,或R 1是氢或可以带有各种取代基的酰基,R 2是 氢或保护基,R3是通式为R'3-SO2-O-或R'3-CO-O-的基团,其中R'3是烷基,三氟甲基,三氯甲基或被取代的苯基 卤素原子或烷基或硝基,R“3定义为R'3,或表示被酰基或烷氧基羰基取代的甲基,或代表在2-位被酰基或烷氧基羰基取代的乙基或丙基。 这些化合物可用作制备抗生素3-硫代乙烯基 - 头孢菌素的中间体。