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    • 12. 发明授权
    • Methods for highly selectively o-alkylating amide compounds with the use of copper salts
    • 使用铜盐高度选择性O-烷基化酰胺化合物的方法
    • US06462195B1
    • 2002-10-08
    • US09622906
    • 2000-09-05
    • Mitsuru TakaseYasuyuki MiyazawaShiro Tsubokura
    • Mitsuru TakaseYasuyuki MiyazawaShiro Tsubokura
    • C07D23952
    • C07D239/52
    • Compounds having one or more structures represented by general formula (I) as partial structure thereof, which are typified by pyrimidone and pyridone compounds, have two or more reaction sites in alkylation reactions. Accordingly, there is no process for producing O-alkylated products of these compounds at a high selectivity or such processes, if any, are applicable exclusively to those having limited structures. A process for selectivity O-alkylating such a compound as described above by converting it into the copper salt by using a monovalent copper compound such as copper suboxide and then reacting it with an alkylating agent having a leaving group in the presence of a phosphorus compound such as a phosphite. Pyrimidyloxy derivatives or pyridyloxy derivatives obtained by this reaction is useful as intermediates of pesticides or drugs.
    • 具有一种或多种由通式(I)表示的结构的化合物作为其部分结构,以嘧啶酮和吡啶酮化合物为代表,在烷基化反应中具有两个或多个反应位点。 因此,没有高选择性地生产这些化合物的O-烷基化产物的方法,或者这些方法(如果有的话)仅专门用于具有有限结构的方法。 通过使用一价铜化合物如低辛氧化物将其转化为铜盐,然后在磷化合物存在下使其与具有离去基团的烷基化剂反应,将上述化合物选择性O-烷基化的方法O-烷基化, 作为亚磷酸酯。 通过该反应获得的嘧啶氧基衍生物或吡啶氧基衍生物可用作农药或药物的中间体。
    • 16. 发明申请
    • NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND METHOD FOR PRODUCING SAME
    • 含氮杂环化合物及其生产方法
    • US20130023664A1
    • 2013-01-24
    • US13638700
    • 2011-03-28
    • Koichi KutoseHiroki InoueShiro Tsubokura
    • Koichi KutoseHiroki InoueShiro Tsubokura
    • C07D213/75C07D213/89
    • C07D213/89C07D213/75
    • There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m≦4.)
    • 提供了可用作农药等的合成中间体的含氮杂环化合物,例如由式(1)表示的取代的氨基 - 吡啶-N-氧化物化合物; 和含氮杂环化合物的制造方法。 (式(1)中,R 1和R 2各自表示氢原子或未取代或取代的烷基; R 3表示氢原子,未取代或取代的烷基羰基等; R 4表示未取代或取代的烷基羰基,未取代的 或取代的芳基羰基等; A表示羟基,硫醇基等; m表示1〜4的整数中的任一个; k表示0〜3的整数中的任一个; k + m< 1l; 4。 )