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    Method for producing n-[4-(6,7-difluoro-2,4-dioxo-1,4-dihydro-2h-quinazoline-3-yl)-phenyl]-acetamide
    5.
    发明专利
    Method for producing n-[4-(6,7-difluoro-2,4-dioxo-1,4-dihydro-2h-quinazoline-3-yl)-phenyl]-acetamide 审中-公开
    生产N- [4-（6,7-二氟-2,4-二氧代-1,4-二氢-2H-喹唑啉-3-基） - 苯基] - 乙酰胺的方法

    公开(公告)号：JP2012162464A

    公开(公告)日：2012-08-30

    申请号：JP2011021873

    申请日：2011-02-03

    Applicant: Sumitomo Seika Chem Co Ltd ,  住友精化株式会社

    Inventor： TANAKA MUNEAKI ,  KUAD PAUL ,  KOBAYASHI TETSUYA ,  ONOZUKA TOMOHIRO

    IPC: C07D239/96

    Abstract: PROBLEM TO BE SOLVED: To provide a method for efficiently producing high-purity N-[4-(6,7-difluoro-2,4-dioxo-1,4-dihydro-2H-quinazoline-3-yl)-phenyl]-acetamide used as an important precursor for production of pharmaceutical intermediates.SOLUTION: In the method for producing N-[4-(6,7-difluoro-2,4-dioxo-1,4-dihydro-2H-quinazoline-3-yl)-phenyl]-acetamide, N-[4-(6,7-difluoro-2,4-dioxo-1,4-dihydro-2H-quinazoline-3-yl)-phenyl]-acetamide is obtained by reacting 2-amino-4,5-difluorobenzoic acid methyl ester with a phenyl chloroformate compound at a predetermined molar ratio, and then, reacting the resultant phenoxy carbonyl amine compound with N-acetyl 1,4-phenylene diamine in a solvent in the presence of a base without performing an isolating process.

    Abstract translation: 待解决的问题：提供一种有效生产高纯度N- [4-（6,7-二氟-2,4-二氧代-1,4-二氢-2H-喹唑啉-3-基） - 苯基] - 乙酰胺用作药物中间体的重要前体。 解决方案：在N- [4-（6,7-二氟-2,4-二氧代-1,4-二氢-2H-喹唑啉-3-基） - 苯基] - 乙酰胺的制备方法中， 得到[4-（6,7-二氟-2,4-二氧代-1,4-二氢-2H-喹唑啉-3-基） - 苯基] - 乙酰胺，通过2-氨基-4,5-二氟苯甲酸甲酯 酯与预定摩尔比的氯甲酸苯酯化合物反应，然后使所得苯氧基羰基胺化合物与N-乙酰基1,4-苯二胺在溶剂中在碱的存在下反应而不进行分离过程。 版权所有（C）2012，JPO＆INPIT

    Method for producing 3-(4-aminophenyl)-6,7-difluoro-1h-quinazoline-2,4-dione and salt thereof, method for producing quinazolinedione derivative useful for the production method, and imine derivative useful for the method for producing quinazolinedione derivative
    7.
    发明专利
    Method for producing 3-(4-aminophenyl)-6,7-difluoro-1h-quinazoline-2,4-dione and salt thereof, method for producing quinazolinedione derivative useful for the production method, and imine derivative useful for the method for producing quinazolinedione derivative 审中-公开
    用于生产3-（4-氨基苯基）-6,7-二氟-1H-喹唑啉-2,4-二酮及其盐的方法，用于生产用于生产方法的喹诺酮衍生物的方法和用于生产方法的有用的衍生物 衍生物衍生物

    公开(公告)号：JP2012149015A

    公开(公告)日：2012-08-09

    申请号：JP2011009769

    申请日：2011-01-20

    Applicant: Sumitomo Seika Chem Co Ltd ,  住友精化株式会社

    Inventor： TANAKA MUNEAKI ,  SATAKE SHUZO ,  ASHIKAWA MASAYASU ,  FUJIMOTO SHOHEI

    IPC: C07D239/96 ,  C07D209/40

    Abstract: PROBLEM TO BE SOLVED: To provide a method for producing a quinazolinedione derivative used as a medicine production intermediate, and to provide an imine derivative which is a production raw material for the quinazolinedione derivative.SOLUTION: In the production method, 5,6-difluoro-3-(4-nitrophenyl imino)-1,3-dihidro-indol-2-one which is an imine derivative is reacted with an oxidizing agent such as peracetic acid, to thereby obtain a nitro group-containing quinazolinedione derivative. Further, in the production method, the nitro group-containing quinazolinedione derivative is reduced, to thereby obtain a quinazolinedione derivative represented by formula (3).

    Abstract translation: 待解决的问题：提供用作药物生产中间体的喹唑酮二酮衍生物的制备方法，提供作为喹唑啉二酮衍生物的生产原料的亚胺衍生物。 解决方案：在制备方法中，将作为亚胺衍生物的5,6-二氟-3-（4-硝基苯基亚氨基）-1,3-二己基 - 吲哚-2-酮与氧化剂如过乙酸 酸，得到含硝基的喹唑啉二酮衍生物。 此外，在制造方法中，将含有硝基的喹唑啉二酮衍生物还原，得到式（3）表示的喹唑啉二酮衍生物。 版权所有（C）2012，JPO＆INPIT

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