Process for the production of kanomycin B derivatives and products
obtained therefrom
    32.
    发明授权
    Process for the production of kanomycin B derivatives and products obtained therefrom 失效
    生产卡那霉素B衍生物的方法及由此获得的产品

    公开(公告)号:US4349666A

    公开(公告)日:1982-09-14

    申请号:US196586

    申请日:1980-10-14

    CPC分类号: C07H15/234 Y02P20/55

    摘要: 3'-Deoxykanamycin B, namely tobramycin is produced in an improved yield with a reduced reaction time under moderate reaction conditions, starting from a penta-N-protected 3'-mono-O-alkyl-, aralkyl- or arylsulfonylated derivative of kanamycin B in which all the 1, 3, 2' and 3"-amino groups and possibly the 6'-amino group have been protected by an arylsulfonyl group, especially tosyl group; the 3'-hydroxyl group of kanamycin B has been alkyl-, aralkyl- or arylsulfonylated; the 4"- and 6"-hydroxyl groups have been blocked with a di-valent hydroxyl-protecting group; and possibly the 4'-hydroxyl group and 6'-amino group have been blocked by being converted into the form of a 4', 6'-cyclic carbamate formed between the 4'-hydroxyl group and the 6'-amino group, by subjecting to a process essentially comprising reaction of said protected kanamycin B derivative with a metal halide for a reaction time of 30 min. to 2 hours at a reaction temperature of 0.degree. C..about.150.degree. C. to produce the corresponding 3'-halo compound, reductive replacement of the 3'-halo group by hydrogen and deprotection.

    摘要翻译: 3-脱氧卡那霉素B,即在中等反应条件下,以5-N保护的3'-单-O-烷基 - 芳烷基 - 或芳基磺酰化衍生物开始,在中等反应条件下,产率提高,产量提高,反应时间缩短。 其中所有1,3,2'和3“ - 氨基和可能的6'-氨基都被芳基磺酰基,尤其是甲苯磺酰基保护; 卡那霉素B的3'-羟基已经是烷基 - ,芳烷基 - 或芳基磺酰化; 4“和6” - 羟基已被二价羟基保护基封闭; 并且可能的4'-羟基和6'-氨基已经通过在4'-羟基和6'-氨基之间形成的4',6'-环状氨基甲酸酯的形式被阻断,通过 进行基本上包含所述受保护的卡那霉素B衍生物与金属卤化物的反应的方法,反应时间为30分钟。 在0℃的反应温度下反应2小时。在150℃降解产生相应的3'-卤代化合物,通过氢还原取代3'-卤代基团并脱保护。

    Novel process for the preparation of
1-N-(alpha-substituted-omega-aminoacyl)-3'-deoxyribostamycin
    33.
    发明授权
    Novel process for the preparation of 1-N-(alpha-substituted-omega-aminoacyl)-3'-deoxyribostamycin 失效
    制备1-N-(α-取代-ω-氨基酰基)-3 {40-去氧孕酮霉素的新方法

    公开(公告)号:US4125706A

    公开(公告)日:1978-11-14

    申请号:US676792

    申请日:1976-04-14

    IPC分类号: C07H15/23 C07H15/20

    CPC分类号: C07H15/23

    摘要: A 1-N-(.alpha.-substituted-.omega.-aminoacyl)-3'-deoxyribostamycin, which is a useful antibiotic active against various drug-resistant bacteria, can be prepared advantageously by a process starting from a protected derivative of ribostamycin in the form of 1,6-carbamate and comprising the 3'-deoxygenation, the splitting of the carbamate linkage and the 1-acylation.

    摘要翻译: 作为抗各种药物抗性细菌的有用的抗生素的1-N-(α-取代的ω-氨基酰基)-3'-脱氧肉豆蔻霉素可以有利地通过以下形式开始制备:以保护的核糖霉素衍生物形式 的1,6-氨基甲酸酯并且包含3'-脱氧,氨基甲酸酯键的分解和1-酰化。

    1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives of
3'-deoxykanamycin A and the production thereof
    34.
    发明授权
    1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives of 3'-deoxykanamycin A and the production thereof 失效
    3 {40-脱氧卡那霉素A的1-N - ({60-羟基 - {107-氨基烷酰基)衍生物及其制备

    公开(公告)号:US4104372A

    公开(公告)日:1978-08-01

    申请号:US678560

    申请日:1976-04-20

    CPC分类号: C07H15/234 Y02P20/55

    摘要: 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-derivatives of 3'-deoxykanamycin A or 6'-N-methyl-3'-deoxykanamycin A are provided as new and useful compounds which are active against gram-negative and gram-positive bacteria, including drug-resistant strains of these bacteria. Examples of these compounds include 1-N-((SR)-.beta.-amino-.alpha.-hydroxypropionyl)-3'-deoxykanamycin A, 1-N-((S)-.gamma.-amino-.alpha.-hydroxybutyryl)-3'-deoxykanamycin A, 1-N-((S)-.delta.-amino-.alpha.-hydroxyvaleryl)-3'-deoxykanamycin A and 1-N-((S)-.gamma.-amino-.alpha.-hydroxybutyryl)-6'-N-methyl-3'-deoxykanamycin A. The compounds may be prepared by selective acylation of the 1-amino group of 3'-deoxykanamycin A or 6'-N-methyl-3'-deoxykanamycin A with a corresponding .alpha.-hydroxy-.omega.-amino-alkanoic acid.

    摘要翻译: 提供3'-脱氧卡那霉素A或6'-N-甲基-3'-脱氧卡那霉素A的1-N-(α-羟基 - ω-氨基烷酰基)衍生物作为对革兰氏阴性和革兰氏阴性菌具有活性的新的有用化合物 阳性细菌,包括这些细菌的耐药菌株。 这些化合物的实例包括1-N - ((SR)-β-氨基-α-羟基丙酰基)-3'-脱氧卡那霉素A,1-N - ((S)-γ-氨基-α-羟基丁酰基) 脱氧卡那霉素A,1-N - ((S)-δ-氨基-α-羟基戊酰基)-3'-脱氧卡那霉素A和1 -N((S)-γ-氨基-α-羟基丁酰基)-6'-N- 甲基-3'-脱氧卡那霉素A.该化合物可以通过将3-脱氧卡那霉素A或6'- N-甲基-3'-脱氧卡那霉素A的1-氨基选择性酰化与相应的α-羟基 - 氨基 - 链烷酸。

    Image pickup apparatus
    40.
    发明申请
    Image pickup apparatus 审中-公开
    摄像设备

    公开(公告)号:US20050147397A1

    公开(公告)日:2005-07-07

    申请号:US11006721

    申请日:2004-12-08

    CPC分类号: G11B31/006

    摘要: In a small size image pickup apparatus, depending upon the opening direction of the lid, a hand strap and the like become obstacles and it becomes difficult to open a disc lid with a large angle. Hence, a disc-like recording medium cannot be attached to and detached from the disc type image pickup apparatus without difficulty. In a disc type image pickup apparatus comprises a table rotating apparatus 35 for rotating a turntable 36 on which a DVD 2 is detachably loaded in the erected state, an optical pickup apparatus 71 capable of recording an information signal of an image corresponding to light of an object inputted through at least a lens apparatus 4 on the DVD 2 rotated by the table rotating apparatus 35, an outer case 5 having a disc compartment portion 6 in which the table rotating apparatus 35 and the optical pickup apparatus 71 are accommodated and in which the turntable 36 being opened to the side surface thereof and a disc lid 7 attached to the outer case 5 so as become freely openable and closable to cover the disc compartment portion 6. A lid rotary shaft portion 39 is provided on the rear portion of the side surface of the outer case 5 to rotatably support the disc lid 7 and the disc lid 0.7 can be rotated around the lid rotary shaft portion 39 in the lateral direction.

    摘要翻译: 在小尺寸图像拾取装置中,根据盖的打开方向,手带等成为障碍物,并且变得难以以大的角度打开盘盖。 因此,盘状记录介质不能轻易地附接到盘式图像拾取装置并从其拆卸。 在一种盘式摄像装置中,包括一台转台装置35,用于旋转DVD 2以竖立状态可拆卸地装载在其上的转盘36;能够记录与光线对应的图像的信息信号的光学拾取装置71; 通过台式旋转装置35旋转的DVD 2上的至少透镜装置4输入的物体,具有容纳台式旋转装置35和光学拾取装置71的盘室部6的外壳5, 转台36向其侧表面敞开,盘盖7安装在外壳5上,以便可自如地打开和关闭以覆盖盘室隔间6。 在外壳5的侧面的后部设置盖旋转轴部39,以可旋转地支撑盘盖7,并且盘盖0.7可以围绕盖旋转轴部39沿横向旋转。