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    • 9. 发明专利
    • METHOD FOR PRODUCING β-KETOAMIDE DERIVATIVE HAVING NITROGEN-CONTAINING HETEROCYCLE
    • 生产具有含氮杂环化合物的β-酮酸衍生物的方法
    • JP2009280510A
    • 2009-12-03
    • JP2008132178
    • 2008-05-20
    • Daicel Chem Ind Ltdダイセル化学工業株式会社
    • KAMURO YOSHIAKITATSUMI JUNRO
    • C07D263/44
    • PROBLEM TO BE SOLVED: To provide a method for producing a β-ketoamide derivative having a nitrogen-containing heterocycle, by which highly pure powder of the derivative can safely be obtained in good operability.
      SOLUTION: Provided is the method for producing the β-ketoamide derivative having the nitrogen-containing heterocycle, characterized by crystallizing the compound represented by formula (1) [wherein, R
      1 is a 1-8C alkyl group; R
      2 is a nitrogen-containing heterocyclic group; R
      3 is an alkoxy group, an aryloxy group, an alkoxycarbonyloxy group, an N-substituted carbamoyl group, an N-substituted sulfamoyl group, an N-acylamino group or an N-sulfonic acid acylamino group; (n) is an integer of 1 to 5; when (n) is an integer of 2 to 5, several R
      3 groups may be identical or different] in a solvent mixture of an alcohol with water. It is preferable to use the alcohol and the water in amounts of 1 to 10 weight times and 0.1 to 3 weight times, respectively, the weight of the compound of formula (1), in the production method.
      COPYRIGHT: (C)2010,JPO&INPIT
    • 待解决的问题:提供一种具有含氮杂环的β-酮酰胺衍生物的制备方法,通过该方法可以安全地获得具有良好可操作性的高纯度衍生物粉末。 解决方案:提供具有含氮杂环的β-酮酰胺衍生物的制备方法,其特征在于使由式(1)表示的化合物结晶[其中,R 1 为1- 8C烷基; R 2 是含氮杂环基; R 3是烷氧基,芳氧基,烷氧羰基氧基,N-取代氨基甲酰基,N-取代氨磺酰基,N-酰氨基或N-磺酸酰氨基; (n)为1〜5的整数, 当(n)为2至5的整数时,在醇与水的溶剂混合物中,几个R 3 SP 3基团可以相同或不同。 在制备方法中,优选使用醇和水分别为式(1)化合物的重量的1至10重量倍和0.1至3重量倍。 版权所有(C)2010,JPO&INPIT