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    PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY
    1.
    发明公开
    PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINER VERBINDUNG MIT艾滋病病毒整合剂HEMMENDER WIRKUNG

    公开(公告)号：EP3127908A3

    公开(公告)日：2017-02-15

    申请号：EP16190894.2

    申请日：2011-08-04

    申请人： SHIONOGI & CO., LTD

    发明人： SUMINO, Yukihito ,  OKAMOTO, Kazuya ,  MASUI, Moriyasu ,  YAMADA, Daisuke ,  IKARASHI, Fumiya

    IPC分类号： C07D498/14 ,  A61K31/5365 ,  A61P31/18 ,  A61P43/00 ,  C07D211/94 ,  C07D213/80

    CPC分类号： C07D498/14 ,  A61K31/5365 ,  C07B2200/13 ,  C07D213/80

    摘要： A process for preparing a compound represented by formula (Y1) or (Y2) [wherein R x is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R 1d is hydrogen, halogen, or the like; R 2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R 4d is a lower alkyl optionally substituted with substituent E, or the like; and R 6d is a lower alkyl group optionally substituted with substituent group E].

    摘要翻译： 使用由式（Y1）或（Y2）表示的吡啶酮衍生物的新方法制备式（Y1）或（Y2）[其中R x为任选取代的碳环基低级烷基等）或其盐的方法 X4）[其中R 1d是氢，卤素等; R 2d是氢，任选被取代基E取代的低级烷基等; R 4d是任选被取代基E取代的低级烷基等; R 6d为任选被取代基组E取代的低级烷基等）。

    PROCESS FOR PRODUCING ALPHA-HYDROXYIMINOPHENYLACETONITRILE
    7.
    发明授权
    PROCESS FOR PRODUCING ALPHA-HYDROXYIMINOPHENYLACETONITRILE 失效
    生产α-羟基亚氨基苯基乙酰丙酮的方法

    公开(公告)号：EP0658542B1

    公开(公告)日：1998-01-14

    申请号：EP94919839.4

    申请日：1994-07-01

    申请人： SHIONOGI & CO., LTD. ,  SUMITOMO CHEMICAL COMPANY LIMITED

    发明人： TAKASE, Akira ,  KAI, Hiroyuki ,  MASUI, Moriyasu ,  MASUMOTO, Katuhisa ,  NAKAMURA, Akihiko ,  KIYOSHIMA, Yujiro ,  SASAKI, Mikio

    IPC分类号： C07C255/62 ,  C07C253/30 ,  C07C323/63 ,  C07C319/20 ,  C07C253/14

    CPC分类号： C07C251/48 ,  C07C253/14 ,  C07C253/30 ,  C07C255/64

    摘要： A process for producing an alpha -hydroxyiminophenylacetonitrile represented by general formula [II], (wherein R , R , R and Z are each as defined in the specification) by reacting a crude nitrile containing a phenylacetonitrile represented by general formula [I], (wherein R , R , R and Z are each as defined in the specification) with an alkyl nitrite in the presence of a base, extracting the reaction mixture with water, and neutralizing the separated water layer with an acid. This process enables target alpha -hydroxyiminophenylacetonitriles to be readily produced in a highly pure form in high yield by extracting the reaction mass with water and neutralizing the separated water layer with an acid.

    摘要翻译： 由通式[II]表示的α-羟基亚氨基苯基乙腈的制备方法（其中R 1，R 2，R 3和Z各自如说明书中所定义）通过使含有苯基乙腈 （其中R 1，R 2，R 3和Z各自如说明书中所定义）与亚硝酸烷基酯在碱存在下反应，将反应混合物用 水，并用酸中和分离的水层。 该方法通过用水萃取反应物并用酸中和分离的水层，使得目标α-羟基亚氨基苯基乙腈容易以高纯度形式高产率地生成。

    PROCESS FOR PRODUCING $g(a)-ALKOXYIMINOPHENYLACETONITRILE DERIVATIVE
    8.
    发明公开
    PROCESS FOR PRODUCING $g(a)-ALKOXYIMINOPHENYLACETONITRILE DERIVATIVE 失效
    生产$ g（a） - 烷氧基亚氨基苯基乙酰丙酮衍生物的方法

    公开(公告)号：EP0658543A1

    公开(公告)日：1995-06-21

    申请号：EP94919840.2

    申请日：1994-07-01

    申请人： SHIONOGI & CO., LTD. ,  SUMITOMO CHEMICAL COMPANY LIMITED

    发明人： TAKASE, Akira ,  KAI, Hiroyuki ,  MASUI, Moriyasu ,  MASUMOTO, Katuhisa ,  NAKAMURA, Akihiko ,  KIYOSHIMA, Yujiro ,  SASAKI, Mikio

    IPC分类号： C07C255/62 ,  C07C253/30 ,  C07C323/63 ,  C07C319/20

    CPC分类号： C07C251/48 ,  C07C253/30 ,  C07C255/61 ,  C07C319/20

    摘要： A process for producing an α-alkoxyiminophenylacetonitrile represented by general formula [III], (wherein R¹, R², R³ and Y are each as defined in the specification) by reacting an alkali metal salt of an α-hydroxyiminophenylacetonitrile, represented by general formula [I], (wherein R¹, R², Y and A are each as defined in the specification) with a dialkyl sulfate represented by the general formula [II]: (R³)₂SO₄, (wherein R³ is as defined in the specification) in the presence of a phase transfer catalyst in a solvent mixture composed of a hydrocarbon solvent and water. It is possible by using the above catalyst and solvent mixture to inhibit the formation of a nitrone derivative as a by-product to thereby produce a highly pure alkoxyimino compound in a high yield.

    摘要翻译： 由通式[Ⅲ]表示的α-烷氧基亚氨基苯基乙腈的制备方法，其中R 1，R 2，R 3和Y各自如说明书中所定义）通过使通式[Ⅰ]代表的α-羟基亚氨基苯基乙腈的碱金属盐与通式[ （其中R 1，R 2，Y和A各自如说明书中所定义）与通式[Ⅱ]代表的二烷基硫酸盐反应：（R 3）2 SO 4（其中R 3如说明书中所定义） 在由烃溶剂和水组成的溶剂混合物中存在相转移催化剂。 通过使用上述催化剂和溶剂混合物抑制作为副产物的硝酮衍生物的形成，从而以高产率生产高纯度的烷氧基亚氨基化合物是可能的。

    PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY
    9.
    发明公开
    PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY 审中-公开
    制备具有HIV整合酶抑制活性的化合物的方法

    公开(公告)号：EP3127908A2

    公开(公告)日：2017-02-08

    申请号：EP16190894.2

    申请日：2011-08-04

    申请人： SHIONOGI & CO., LTD

    发明人： SUMINO, Yukihito ,  OKAMOTO, Kazuya ,  MASUI, Moriyasu ,  YAMADA, Daisuke ,  IKARASHI, Fumiya

    IPC分类号： C07D498/14 ,  A61K31/5365 ,  A61P31/18 ,  A61P43/00 ,  C07D211/94 ,  C07D213/80

    CPC分类号： C07D498/14 ,  A61K31/5365 ,  C07B2200/13 ,  C07D213/80

    摘要： A process for preparing a compound represented by formula (Y1) or (Y2) [wherein R x is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R 1d is hydrogen, halogen, or the like; R 2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R 4d is a lower alkyl optionally substituted with substituent E, or the like; and R 6d is a lower alkyl group optionally substituted with substituent group E].

    摘要翻译： （Y1）或（Y2）[其中Rx为任选取代的碳环基低级烷基等]代表的化合物或其盐的方法，或其盐，采用制备式（X4）代表的吡啶酮衍生物 ）[其中R1d是氢，卤素等; R2d是氢，任选被取代基E取代的低级烷基等; R4d是任选被取代基E取代的低级烷基，等等; 和R6d是任选被取代基E取代的低级烷基]。