2',3'-dideoxy-2'-fluorokanamycin A and
1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof
    7.
    发明授权
    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及其1-N-(α-羟基-ω-氨基烷酰基)衍生物

    公开(公告)号:US4661474A

    公开(公告)日:1987-04-28

    申请号:US807485

    申请日:1985-12-10

    CPC分类号: C07H15/234 Y02P20/55

    摘要: New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryl)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as antibacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-O-protected-2,3,6-trideoxy-2-fluoro-.alpha.-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-O-(2',4',6'-tri-O-protected-3'-N-protected-3'-amino-3'-deoxy-.alpha.-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.

    摘要翻译: 新化合物2',3'-二脱氧-2'-氟卡那霉素A及其1-N-(α-羟基-ω-氨基烷酰基)衍生物,特别是1-N-(DL-或L-3-氨基-2- 羟基丙酰基) - 和1-N-(L-4-氨基-2-羟基丁酰基)-2',3'-二脱氧-2'-氟吗啉霉素A,其各自可用作抗菌剂。 2',3'-二脱氧-2'-氟卡那霉素A通过以下方法制备,该方法包括将6-叠氮基-4-O-保护的2,3,6-三脱氧-2-氟-α-D-吡喃六氟肉豆蔻基 溴化物与6-O-(2',4',6'-三-O-保护的3'-N-保护的-3'-氨基-3'-脱氧-α-D- D-吡喃葡萄糖基)-1,3-双-N-保护的2-脱氧链霉胺,将所得缩合产物还原,将其叠氮基转化为氨基,并从还原产物中除去剩余的氨基保护基和羟基保护基团。

    "> 3
    8.
    发明授权
    3"-Deoxystreptomycin production thereof and pharmaceutical compositions containing same 失效
    3“ - 其中含有霉菌霉素及含有它们的药物组合物

    公开(公告)号:US4473557A

    公开(公告)日:1984-09-25

    申请号:US475269

    申请日:1983-03-09

    CPC分类号: C07H15/238 Y02P20/55

    摘要: A new semi-synthetic antibiotic, 3"-deoxystreptomycin is now provided, which is useful as an antibacterial agent and is produced from 3"-deoxydihydrostreptomycin by a process comprising oxidizing the 3'-hydroxymethyl group of 2,5,6,4",6"-penta-O-acetyl-2"-N-benzyloxycarbonyl-3"-deoxydihydrostreptomycin as prepared by skilled introduction of amino-protecting group and hydroxyl-protecting group of appropriately selected natures into 3"-deoxydihydrostreptomycin, and then removing the protective groups from the oxidation product, 2,5,6,4",6"-penta-O-acetyl-2"-N-benzyloxycarbonyl-3"-deoxystreptomycin.

    摘要翻译: 现在提供一种新的半合成抗生素3'-脱氧链霉素,其可用作抗菌剂并且由3'-脱氧双氢链霉素通过包括氧化2,5,6的3'-羟甲基的方法制备, 4“,6” - 五-O-乙酰基-2“ - N-苄氧羰基-3” - 脱氧二氢嘧啶霉素,由熟练引入氨基保护基和适当选择的性质的羟基保护基制成3' 脱氧链霉素,然后从氧化产物2,5,6,4',6“ - 五-O-乙酰基-2”-N-苄氧羰基-3“ - 脱氧链霉素中除去保护基团。

    1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin
and the production thereof
    9.
    发明授权
    1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin and the production thereof 失效
    1-N - ((S) - {60-取代的 - {107-氨基酰基) - 纳米颗粒或 - 瑞波霉素及其制备

    公开(公告)号:US4008362A

    公开(公告)日:1977-02-15

    申请号:US390217

    申请日:1973-08-21

    CPC分类号: C07H15/224 C07H15/23

    摘要: An 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula ##STR1## wherein R is a hydrogen atom or .beta.-D-ribofuranosyl group of the formula ##STR2## and R.sub.3 is hydroxyl, amino-NH.sub.2 or acylamino group --NHR.sub.4 in which R.sub.4 is an acyl group, and n is a whole number of 1 to 4, may be produced by subjecting the corresponding O-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula ##STR3## or its hydroxyl-masked and maino-masked form, to the action of a basic medium to produce an acyl-migration product of the formula: ##STR4## and, optionally converting the amino-masking groups into hydrogen atoms and also the hydroxyl-masking group into hydroge atom in a known manner if said amino-masking groups and said hydroxyl-masking groups are present in the acyl-migration product. The 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin produced is characterized by its useful activity inhibitory to the growth of bacteria resistant to the parent substance neamine or ribostamycin.

    摘要翻译: 式(1)的1-N - ((S)-α-取代的ω-氨基酰基) - 单胺或-ribostamycin,其中R为氢原子或式为“IMAGE”的β-D-呋喃核糖基,R3为 是其中R 4为酰基,n为整数1至4的羟基,氨基-NH 2或酰基氨基-NHR 4,其可以通过使相应的O - ((S)-α-取代的ω- 氨基酰基) - 奈米霉素或结晶霉素或其羟基掩蔽和主掩蔽形式,与碱性介质的作用产生下式的酰基迁移产物:和/或将 如果所述氨基掩蔽基团和所述羟基掩蔽基团存在于酰基迁移产物中,则以已知方式将氨基掩蔽基团转化成氢原子,并将羟基掩蔽基团转变成水解原子。 产生的1-N - ((S)-α-取代的ω-氨基酰基) - 单胺或 - 生物素 - 特异霉素的特征在于其对母体neamine或核糖霉素具有抗性的细菌的生长有抑制作用。

    1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin
and the production thereof
    10.
    发明授权
    1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin and the production thereof 失效
    1-N - ((S) - {60-取代的 - {107-氨基酰基) - 纳米颗粒或 - 瑞波霉素及其制备

    公开(公告)号:US4008218A

    公开(公告)日:1977-02-15

    申请号:US559771

    申请日:1975-03-19

    CPC分类号: C07H15/224 C07H15/23

    摘要: An 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula: ##STR1## wherein R is a hydrogen atom or .beta.-D-ribofuranosyl group of the formula ##STR2## and R.sub.3 is hydroxyl, amino-NH.sub.2 or acylamino group --NHR.sub.4 in which R.sub.4 is an acyl group, and n is a whole number of 1 to 4, may be produced by subjecting the corresponding O-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula ##STR3## or its hydroxyl-masked and amino-masked form, to the action of a basic medium to produce an acyl-migration product of the formula: ##STR4## and, optionally converting the amino-masking groups into hydrogen atoms and also the hydroxyl-masking group into hydrogen atom in a known manner if said amino-masking groups and said hydroxyl-masking groups are present in the acyl-migration product. The 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin produced is characterized by its useful activity inhibitory to the growth of bacteria resistant to the parent substance neamine or ribostamycin.

    摘要翻译: 具有下式的1-N - ((S)-α-取代的ω-氨基酰基) - 微量胺或 - 瑞波霉素:其中R是式“IMAGE”的氢原子或β-D-呋喃核糖基, R 3是羟基,氨基-NH 2或酰基氨基-NHR 4,其中R 4是酰基,n是整数1至4,可以通过使相应的O - ((S)-α-取代的-ω- - 氨基酰基) - 或者其羟基掩蔽和氨基掩蔽形式的微生物胺或β-内啡霉素或碱性培养基,以产生下式的酰基迁移产物: 如果所述氨基掩蔽基团和所述羟基掩蔽基团存在于酰基迁移产物中,则以已知的方式将氨基掩蔽基团转化成氢原子,并将羟基掩蔽基团转变为氢原子。 产生的1-N - ((S)-α-取代的ω-氨基酰基) - 单胺或 - 生物霉素的特征在于其对母体neamine或核糖霉素具有抗性的细菌的生长有抑制作用。