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    Process for producing 5-perfluoroalkyluracil derivatives
    5.
    发明授权
    Process for producing 5-perfluoroalkyluracil derivatives 有权
    生产5-全氟烷基尿嘧啶衍生物的方法

    公开(公告)号：US6087499A

    公开(公告)日：2000-07-11

    申请号：US129344

    申请日：1998-08-05

    申请人： Kazuhiko Tokoyoda ,  Koji Kato ,  Masami Takemitsu ,  Hiroaki Mizumoto ,  Shoji Arai

    发明人： Kazuhiko Tokoyoda ,  Koji Kato ,  Masami Takemitsu ,  Hiroaki Mizumoto ,  Shoji Arai

    IPC分类号： C07D239/22 ,  C07D239/02

    CPC分类号： C07D239/22

    摘要： A novel process is provided for producing a 5-perfluoroalkyl-5,6-dihydrouracil represented by General Formula (1): ##STR1## (where R.sup.1 and R.sup.2 are independently hydrogen, methyl, or ethyl, and Rf is a perfluoroalkyl of 1 to 10 carbons). The process comprises reacting .alpha.-perfluoroalkylacrylic acid represented by General Formula (2):CH.sub.2 =C(Rf)--COOH (2)with a urea derivative represented by General Formula (3):R.sup.1 NHCONHR.sup.2 (3)in the presence of acetic anhydride with formed acetic acid being removed out of the reaction system during the reaction. The .alpha.-perfluoroalkylacrylic acid may be added successively. A process for producing a 5-perfluoroalkyl-5-bromo-6-hydrouracil by General Formula (4) is also provided: ##STR2## (where R.sup.1, R.sup.2, and Rf are as defined above) wherein the reaction of a 5-perfluoroalkyl-5,6-dihydrouracil produced by the above process with bromine is conducted in water as the solvent. The process of the present invention can be industrially conducted safely and simply at a high yield.

    摘要翻译： 提供了用于制备由通式（1）表示的5-全氟烷基-5,6-二氢尿嘧啶的新方法：（其中R 1和R 2独立地是氢，甲基或乙基，R f是1至10个碳的全氟烷基） 。 该方法包括使由通式（2）表示的α-全氟代烷基丙烯酸：CH2 = C（Rf）-COOH（2）与通式（3）表示的脲衍生物：R1NHCONHR2（3）在乙酸酐存在下反应， 在反应期间将形成的乙酸从反应体系中除去。 可以连续加入α-全氟烷基丙烯酸。 还提供了通式（4）制备5-全氟烷基-5-溴-6-氢尿嘧啶的方法：（其中R1，R2和Rf如上定义），其中5-全氟烷基-5， 通过上述方法用溴制备的6-二氢尿嘧啶在水中作为溶剂进行。 本发明的方法可以在工业上以高产率安全和简单地进行。