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    Process for the production of 3'-deoxykanamycin A and intermediate product
    2.
    发明授权
    Process for the production of 3'-deoxykanamycin A and intermediate product 失效
    制备3'-脱氧卡那霉素A和中间产物的方法

    公开(公告)号：US4359572A

    公开(公告)日：1982-11-16

    申请号：US256131

    申请日：1981-04-21

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta

    IPC分类号： C07H15/234 ,  C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234 ,  Y02P20/55

    摘要： 3'-Deoxykanamycin A useful as an antibacterial agent can be produced by a new process comprising reacting a 2',2"-di-O-acylated-3'-O-sulfonylated-tetra-N-protected derivative of kanamycin A with a base such as alkali metal alcoholate in a lower alkanol to effect 2',3'- and 3',4'-epoxidation and concurrently removal of the 2'- and 2"-acyl groups, reducing the resultant N-protected 2',3'-anhydro-3'-epi derivative and 3',4'-anhydro-3'-epi derivative of kanamycin A either with hydrogen in the presence of a known hydrogenation catalyst or with sodium borohydride to afford the corresponding N-protected 3'-deoxygenated derivative of kanamycin A and then removing the residual amino-protecting groups therefrom to give 3'-deoxykanamycin A.

    摘要翻译： 可用作抗菌剂的3'-脱氧卡那霉素A可以通过新的方法制备，包括使卡那霉素A的2'，2“ - 二-O-酰化-3'-O-磺酰化四-N-保护的衍生物与 碱如碱金属醇化物在低级链烷醇中进行2'，3'和3'，4'-环氧化并同时去除2'-和2“ - 酰基，将所得N-保护的2 '，3'-脱水-3'-外延衍生物和卡那霉素A的3'，4'-脱氢-3'-epi衍生物，与已知氢化催化剂或硼氢化钠存在下的氢气反应，得到相应的N- 保护的卡那霉素A的3'-脱氧衍生物，然后从其中除去残留的氨基保护基，得到3'-脱氧卡那霉素A.

    Derivative of kanamycin A and a process for the preparation thereof
    5.
    发明授权
    Derivative of kanamycin A and a process for the preparation thereof 失效
    卡那霉素A的衍生物及其制备方法

    公开(公告)号：US4337336A

    公开(公告)日：1982-06-29

    申请号：US235576

    申请日：1981-02-18

    申请人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta ,  Tadashi Wakazawa

    发明人： Hamao Umezawa ,  Sumio Umezawa ,  Shunzo Fukatsu ,  Toshio Yoneta ,  Tadashi Wakazawa

    IPC分类号： C07H15/234 ,  C07H15/236 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/234

    摘要： There are provided new compounds, 3',4'-anhydro-4'-epi derivatives of kanamycin A of the formula: ##STR1## wherein R represents an alkyl, aralkyl or aryl group and Y represents an alkylidene, aralkylidene, cycloalkylidene or tetrahydropyranylidene group which are useful as an intermediate for the synthesis of 3',4'-dideoxykanamycin A and 4'-deoxykanamycin A from kanamycin A. The compounds of formula (I) can be prepared by treating the corresponding 4'-O-sulfonyl derivative with an alkali metal alcoholate in a lower alkanol under an alkaline condition.

    摘要翻译： 提供了下式的卡那霉素A的新化合物3'，4'-脱水-4'-表面衍生物：其中R表示烷基，芳烷基或芳基，Y表示亚烷基，亚烷基， 可用作合成来自卡那霉素A的3'，4'-二脱氧卡那霉素A和4'-脱氧卡那霉素A的中间体的环亚烷基或四氢吡喃亚基。式（I）化合物可以通过将相应的4'- 磺酰基衍生物与碱金属醇化物在低级烷醇中在碱性条件下反应。

    Process for the production of 4-aminobutyric acid or its derivatives
    8.
    发明授权
    Process for the production of 4-aminobutyric acid or its derivatives 失效
    生产4-氨基丁酸或其衍生物的方法

    公开(公告)号：US4290972A

    公开(公告)日：1981-09-22

    申请号：US92940

    申请日：1979-11-09

    申请人： Toshio Yoneta ,  Seiji Shibahara ,  Shigeo Seki ,  Shunzo Fukatsu

    发明人： Toshio Yoneta ,  Seiji Shibahara ,  Shigeo Seki ,  Shunzo Fukatsu

    IPC分类号： C07C227/04 ,  A61K31/19 ,  C07B31/00 ,  C07C20060101 ,  C07C67/00 ,  C07C227/00 ,  C07C227/06 ,  C07C227/26 ,  C07C229/04 ,  C07C229/06 ,  C07C229/22 ,  C07C229/26 ,  C07C99/10 ,  C07C121/42 ,  C07C121/453

    CPC分类号： C07C255/00 ,  Y02P20/55

    摘要： 4-Amino-2-hydroxybutyric acid or 2,4-diaminobutyric acid may be readily produced by a new process comprising reacting a propionic acid compound containing a .beta.-carboxamido substituent (-CONH.sub.2) on the carbon atom at the 3-position and optionally containing hydroxyl substituent and protected or unprotected amino substituent on the .alpha.-carbon atom thereof, with an alkanoic acid anhydride in liquid pyridine to convert the carboxamido group into a nitrile group, with occasional acylation of a .alpha.-hydroxyl group, occasionally removing the alkanoyl group from the .alpha.-acyloxyl group of the resulting nitrile intermediate, and then reducing the resultant nitrile compound with hydrogen to convert the nitrile group into an aminomethyl group, and further optionally removing the residual amino-protecting group from the resultant 4-aminobutyric acid compound.

    摘要翻译： 4-氨基-2-羟基丁酸或2,4-二氨基丁酸可以通过一种新方法容易地产生，包括使含有β-羧酰胺基取代基（-CONH 2）的丙酸化合物在3-位上的碳原子上和任选地 在其α-碳原子上含有羟基取代基和被保护或未被保护的氨基取代基，与链烷酸酐在液体吡啶中，将羧酰胺基转化为腈基，偶尔酰化α-羟基，偶尔除去烷酰基 由得到的腈中间体的α-酰氧基，然后用氢还原得到的腈化合物，将腈基转化为氨基甲基，进一步任选地从所得的4-氨基丁酸化合物中除去残留的氨基保护基。