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203 条记录 (耗时 0.025 秒)

    3'-Fluoro-3'-deoxykanamycin a and the production thereof
    71.
    发明公开
    3'-Fluoro-3'-deoxykanamycin a and the production thereof 失效
    3'-氟 - 3'-脱氧肉桂酸A及其生产方法

    公开(公告)号：EP0173614A3

    公开(公告)日：1986-08-13

    申请号：EP85401575

    申请日：1985-08-01

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Umezawa, Hamao ,  Umezawa, Sumio ,  Tsuchiya Tsutomu ,  Takahashi, Yoshiaki

    IPC分类号： C07H15/234 ,  A61K31/70 ,  C07H09/04

    CPC分类号： C07H15/234 ,  C07H9/04 ,  Y02P20/55

    摘要： A new compound, 3'-fluoro-3'-deoxykanamycin A is now provided, which is active against gram-negative and gram-positive bacteria, including kanamycin-resistant strains of bacteria and is useful as antibacterial agent for therapeutic treatment of bacterial infections. This new compound is produced by a process comprising reacting a 6- azido-2,4-di-O-protected-3,6-dideoxy-3-fluoro-α-D-glucopyranosyl bromide with the 4-hydroxyl group of a 6-0-(2'-0- protected-3'-N-protected-3'-amino-4',6'-di-O-protected-3'-deoxy-a-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the azido group of the resulting reaction product into an amino group, and removing the remaining protective groups from the reduction product.

    2',3'-Dideoxy-2'-fluorokanamycin A and 1-N-(alpha-hydroxy-omega-aminoalkanoyl) derivatives thereof
    73.
    发明公开
    2',3'-Dideoxy-2'-fluorokanamycin A and 1-N-(alpha-hydroxy-omega-aminoalkanoyl) derivatives thereof 失效
    2'，3'-二脱氧-2'-氟卡那霉素-A和Seine 1-N-（α-羟基-ω-氨基烷酰基）-Derivate。

    公开(公告)号：EP0185323A2

    公开(公告)日：1986-06-25

    申请号：EP85115901.2

    申请日：1985-12-13

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Umezawa, Hamao ,  Umezawa, Sumio ,  Tsuchiya, Tsutomu ,  Takahashi, Yoshiaki

    IPC分类号： C07H15/236 ,  C07H15/234 ,  A61K31/70

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(a-hydroxy-w-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryt)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as anti-bacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-0-protected-2,3-6-trideoxy-2-fluoro-a-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-0-(2',4',6'-tri-0- protected-3'-N-protected-3'-amino-3'-deoxy-α-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the resulting condensation product to convert its azido group into an amino group, and removing the remaining amino-protecting and hydroxyl-protecting groups from the reduction product.

    New processes for the production of di-alkyl esters and optically active mono-alkyl esters of 3-aminoglutaric acid
    76.
    发明公开
    New processes for the production of di-alkyl esters and optically active mono-alkyl esters of 3-aminoglutaric acid 失效
    Verfahren zur Produktion von Di-alkylestern und optisch aktiven Mono-alkylestern von 3-Aminoglutarsäure。

    公开(公告)号：EP0050799A1

    公开(公告)日：1982-05-05

    申请号：EP81108343.5

    申请日：1981-10-15

    申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI

    发明人： Ohno, Masaji ,  Umezawa, Hamao

    IPC分类号： C07C101/20 ,  C07C99/00 ,  C07C125/065 ,  C09B19/00

    CPC分类号： C12P41/005 ,  C07C227/06

    摘要： A new process is provided for the production of a di-alkyl 3-aminoglutarate which are found useful as intermediates for the synthesis of β-lactam antibiotics of carbapenem type such as thienamycin. The new process comprises reacting an ammonium salt or ammonia with a di-alkyl ester of 3- ketoglutaric acid to form unsaturated amine compounds and reducing the latter with an alkali metal cyanoborohydride. The N-protected derivative of di-alkyl 3-aminoglutarate prepared may be converted into the optically active p-(S)-mono-alkyl half ester by treatment with esterase to hydrolyze only one of the esters (pro-R ester), followed by conventional N-deprotection. Further, di-alkyl 3-aminoglutarate itself may immediately be converted into the optically active β-(R)-mono-alkyl half ester of 3-aminoglutaric acid by treatment with esterase to hydrolyze preferentially one ester-forming alkyl group (pro-S ester).

    摘要翻译： 提供了用于生产3-氨基戊二酸二烷基酯的新方法，其可用作合成碳青霉烯类型的β-内酰胺抗生素如噻吩霉素的中间体。 新方法包括使铵盐或氨与3-酮戊二酸的二烷基酯反应以形成不饱和胺化合物，并用碱金属氰基硼氢化物还原后者。 所制备的N-烷基3-氨基戊二酸的N-保护的衍生物可以通过用酯酶处理而转化成光学活性的β-（S） - 单烷基半酯，以仅水解酯（前酯酯），然后常规 的N-脱保护。 此外，3-氨基戊二酸二烷基本身可以立即通过用酯酶处理而被转化为3-氨基戊二酸的光学活性β-（R） - 单烷基半酯，以优先水解一个酯形成烷基（亲-S 酯）。