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17 条记录 (耗时 0.026 秒)

    Process for 1-carba(dethia) cephalosporins
    6.
    发明授权
    Process for 1-carba(dethia) cephalosporins 失效
    1-carba（dethia）头孢菌素的方法

    公开(公告)号：US4939249A

    公开(公告)日：1990-07-03

    申请号：US245185

    申请日：1988-09-16

    申请人： Larry C. Blaszczak

    发明人： Larry C. Blaszczak

    IPC分类号： C07D487/04 ,  C07D205/085 ,  C07D463/00 ,  C07D501/14 ,  C07F7/18

    CPC分类号： C07D205/085 ,  C07D463/04 ,  C07D463/06

    摘要： The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics represented by the formula ##STR1## wherein R is amino or protected amino, R.sub.1 is H or alkoxy, R.sub.3 is H or alkyl, Z is ##STR2## where R.sub.2 is, e.g., H, halogen, or alkyl, or --CH.sub.2 R.sub.2 ' where R.sub.2 ' is, e.g., hydroxy, methoxy, or heterocyclicthio group, and A is a carboxy-protecting group which comprises heating a 2-substituted-methylcephalosporin 1,1-dioxide of the formula ##STR3## wherein R, R.sub.1, R.sub.3, and A are the same as in the formula above and Y is a free radical precursor group, e.g., C.sub.1 -C.sub.6 --Se--, C.sub.1 -C.sub.6 --S--, or phenyl--Se--; with a free radical initiator, e.g., a trialkyltin hydride, radiation, or a cobalt I salophen. Also provided are free radical compounds formed as intermediates in the process.

    Cephalosporin free radical compounds
    8.
    发明授权
    Cephalosporin free radical compounds 失效
    头孢菌素自由基化合物

    公开(公告)号：US5037975A

    公开(公告)日：1991-08-06

    申请号：US500326

    申请日：1990-03-28

    申请人： Larry C. Blaszczak

    发明人： Larry C. Blaszczak

    IPC分类号： C07D205/085 ,  C07D463/00 ,  C07D501/14

    CPC分类号： C07D205/085 ,  C07D463/20

    摘要： The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics with 2-substituted methylcephalosporin 1,1-dioxides wherein the substituent on the 2-methylene group is a free radical precursor group such as a phenyl or alkylseleno group. The latter dioxides are treated with a free radical initiator, e.g., a trialkyltin hydride or actinic radiation at 40.degree. C. to 150.degree. C. to provide the 1-carba-3-cephem and 1-carba-2-cephem products. The invention also provides free radical compounds formed as intermediates in the process.

    摘要翻译： 本发明提供了用2-取代甲基头孢菌素1,1-二氧化物制备1-咔唑（1-脱氢）头孢菌素抗生素的自由基方法，其中2-亚甲基上的取代基是自由基前体基团，例如苯基或烷基硒 组。 后者的二氧化物用自由基引发剂如氢化三烷基锡或光化辐射在40℃至150℃下进行处理以提供1-咔唑-3-头孢烯和1-咔二-2-头孢烯产物。 本发明还提供了在该方法中作为中间体形成的自由基化合物。

    Method of deprotection of 3-amino azetidinones
    9.
    发明授权
    Method of deprotection of 3-amino azetidinones 失效
    3-氨基氮杂环丁酮脱保护方法

    公开(公告)号：US4983732A

    公开(公告)日：1991-01-08

    申请号：US410208

    申请日：1989-09-21

    申请人： Larry C. Blaszczak ,  John E. Munroe ,  Douglas O. Spry

    发明人： Larry C. Blaszczak ,  John E. Munroe ,  Douglas O. Spry

    IPC分类号： C07D205/085 ,  C07D463/00 ,  C07D501/22 ,  C07D505/00

    CPC分类号： C07D505/00 ,  C07D205/085 ,  Y02P20/55

    摘要： A method for preparing 2-amino-.beta.-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-.beta.-lactam is further acylated with a different acyl group and is subsequently treated with base to provide a protected 2-amino .beta.-lactam with allyloxycarbonyl, t-butoxycarbonyl, naphthyloxycarbonyl, trichloroethyloxycarbonyl, p-nitrobenzyloxycarbonyl, benzhydryloxycarbonyl, p-methoxybenzyloxycarbonyl, or o-nitrobenzyloxycarbonyl.

    摘要翻译： 提供了由容易去除的保护基团取代的制备2-氨基-β-内酰胺的方法。 根据本发明，酰基-2-氨基-β-内酰胺进一步用不同的酰基进行酰化，随后用碱处理以提供受保护的2-氨基β-内酰胺与烯丙氧基羰基，叔丁氧基羰基，萘氧基羰基，三氯乙氧基羰基， 对硝基苄氧羰基，二苯甲氧基羰基，对甲氧基苄氧羰基或邻硝基苄氧羰基。