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    PROCESSES FOR THE PREPARATION OF PYRIDINE DERIVATIVES
    3.
    发明授权
    PROCESSES FOR THE PREPARATION OF PYRIDINE DERIVATIVES 失效
    用于生产吡啶

    公开(公告)号：EP0997461B1

    公开(公告)日：2003-05-21

    申请号：EP98931055.2

    申请日：1998-07-10

    申请人： Eisai Co., Ltd.

    发明人： TAGAMI, Katsuya ,  NIIKAWA, Nobuo ,  KAYANO, Akio ,  KURODA, Hirofumi

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12

    摘要： Processes for preparing sulfoxides useful as drugs such as acid secretion inhibitors or antiulcer drugs or intermediates for the preparation of drugs in high yields, at high purities, and with safety. Specifically, a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with a peroxoborate salt in the presence of an acid anhydride or a metal catalyst; and a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with an N-halosuccinimide, 1,3-dihalo-5,5-dimethyl-hydantoin or dichloroisocyanuric acid salt in the presence of a base. In said formulae R1 is hydrogen, methoxy or difluoromethoxy; R2 is methyl or methoxy; R3 is 3-methoxypropoxy, methoxy or 2,2,2-trifluoroethoxy; and R4 is hydrogen or methyl.

    PROCESSES FOR THE PREPARATION OF PYRIDINE DERIVATIVES
    6.
    发明公开
    PROCESSES FOR THE PREPARATION OF PYRIDINE DERIVATIVES 失效
    VERFAHREN ZUR HERSTELLUNG VON PYRIDINDERIVATEN

    公开(公告)号：EP0997461A1

    公开(公告)日：2000-05-03

    申请号：EP98931055.2

    申请日：1998-07-10

    申请人： Eisai Co., Ltd.

    发明人： TAGAMI, Katsuya ,  NIIKAWA, Nobuo ,  KAYANO, Akio ,  KURODA, Hirofumi

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12

    摘要： The present invention provides a method for producing sulfoxide useful as medicaments such as inhibitors of gastric acid secretion, anti-ulcer agents etc., or as intermediates for producing medicaments, at a high yield and a high purity in a safe manner.
    A method for producing sulfoxide (II), comprising the step of oxidizing thioether (I) in the presence of an acid anhydride or a metal catalyst with a perborate, or a method for producing sulfoxide (II), comprising the step of oxidizing thioether (I) in the presence of a base with N-halosuccinimide, 1,3-dihalo-5,5-dimethylhydantoin or a dichloroisocyanurate:
    wherein R 1 is a hydrogen atom, a methoxy group or a difluoromethoxy group; R 2 is a methyl group or a methoxy group; R 3 is a 3-methoxypropoxy group, a methoxy group or a 2,2,2-trifluoroethoxy group; and R 4 represents a hydrogen atom or a methyl group.

    摘要翻译： 本发明提供了一种生产亚硫酸盐的方法，其用作药物如胃酸分泌抑制剂，抗溃疡剂等，或作为制备药物的中间体，以高产率和高纯度安全地生产。 一种生产亚砜（II）的方法，包括在酸酐或金属催化剂存在下用过硼酸盐氧化硫醚（I）的步骤或其制备亚砜（II）的方法，其包括将硫醚（ I）在碱存在下与N-卤代琥珀酰亚胺，1,3-二卤代-5,5-二甲基乙内酰脲或二氯异氰脲酸酯的存在：其中R 1为氢原子，甲氧基或二氟甲氧基; R 2是甲基或甲氧基; R 3是3-甲氧基丙氧基，甲氧基或2,2,2-三氟乙氧基; R 4表示氢原子或甲基。

    PHOSPHORUS-SUBSTITUTED ISOPRENOID DERIVATIVE
    9.
    发明公开
    PHOSPHORUS-SUBSTITUTED ISOPRENOID DERIVATIVE 失效
    磷酸二氢钠

    公开(公告)号：EP0609440A1

    公开(公告)日：1994-08-10

    申请号：EP92918492.7

    申请日：1992-08-27

    申请人： Eisai Co., Ltd.

    发明人： TAGAMI, Katsuya ,  YOSHIDA, Ichiro ,  KOBAYASHI, Naoki ,  FUKUDA, Yoshio ,  EGUCHI, Yoshihito ,  NAKAGAWA, Makoto ,  HIYOSHI, Hironobu ,  IKUTA, Hironori ,  KAINO, Makoto ,  HAYASHI, Kenji ,  OHTSUKA, Issei ,  ABE, Shinya ,  SOUDA, Shigeru

    IPC分类号： C07F9/38 ,  C07F9/40 ,  A61K31/66

    CPC分类号： C07F9/405 ,  C07C211/21 ,  C07C233/03 ,  C07F9/3808 ,  C07F9/3826 ,  C07F9/3843 ,  C07F9/3873 ,  C07F9/4006 ,  C07F9/4015 ,  C07F9/4025

    摘要： A phosphorus-substituted isoprenoid derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, useful for preventing and treating diseases for which a squalene synthetase inhibition is efficacious. In formula (I), R¹ and R² represent each hydrogen, lower alkyl, cycloalkyl, alkenyl, alkynyl, aryl which may be substituted, arylalkyl which may be substituted on the aryl moiety, heteroaryl or heteroarylalkyl; R³ and R⁴ represent each hydrogen, lower alkyl or alkali metal; Y represents -P(O)(OR⁵)(OR⁶) (wherein R⁵ and R⁶ represent each hydrogen, lower alkyl or alkali metal) or -CO₂R⁷ (wherein R⁷ represents hydrogen, lower alkyl or alkali metal); Z represents -(CH₂) m - (wherein m represents an integer of 0 or 1 to 3), -(CH₂) p -CH=CH-(CH₂) q - (wherein m represents 0 or 1 and q represents 1 or 2), or -A-NR⁸-(CH₂) r - (wherein R⁸ represents hydrogen or lower alkyl, A represents C₁ to C₅ alkylene, and r represents an integer of 0 or 1 to 5); and n represents an integer of 0 or 1 to 5.

    摘要翻译： 用于预防和治疗角鲨烯合成酶抑制有效的疾病的通式（I）表示的磷取代的类异戊二烯衍生物或其药理学上可接受的盐。 在式（I）中，R 1和R 2分别代表氢，低级烷基，环烷基，烯基，炔基，可被取代的芳基，可在芳基部分上被取代的芳基烷基，杂芳基或杂芳基烷基; R 3和R 4各自代表氢，低级烷基或碱金属; Y表示-P（O）（OR 5）（OR 6）（OR 6）（其中R 5和R 6表示每个氢，低级烷基或碱金属）或-CO 2 R 7（其中R' 7>代表氢，低级烷基或碱金属）; Z表示 - （CH 2）m - （其中m表示0或1〜3的整数）， - （CH 2）p -CH = CH-（CH 2）q - （其中m表示0或1，q表示1或2 ）或-A-NR 8 - （CH 2）r - （其中R 8表示氢或低级烷基，A表示C 1至C 5亚烷基，r表示0或1至5的整数）; n表示0或1〜5的整数