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    • 1. 发明专利
    • (p-hydroxyphenyl)(perfluoroalkyl)acetonitrile derivative
    • (对羟基苯基)(全氟代苄基)乙酸衍生物
    • JPS5927862A
    • 1984-02-14
    • JP13734282
    • 1982-08-09
    • Sagami Chem Res Center
    • UMEMOTO TERUOMIYANO OSAMU
    • C07C69/732C07C39/24C07C51/00C07C59/56C07C67/00C07C253/00C07C255/31C07C255/36
    • NEW MATERIAL:The compound of formula I (Rf is lower perfluoroalkyl; R is H or tertiary alkyl).
      EXAMPLE: 4-(1'-Cyano-2',2',2'-trifluoroethyl)-2,6-di-t-butylphenol.
      USE: A synthetic intermediate of p-hydroxyphenyl-α-trifluoromethyl-acetic acid or its ester useful as a modifier of cephalosporin.
      PROCESS: The compound of formula I can be prepared by the catalytic hydrogenation of the quinone compound of formula II in the presence of a reduction catalyst (e.g. Pd/C). The reaction is preferably carried out in a solvent (e.g. acetonitrile) at 0W60°C. A compound of formula I wherein R is tert-alkyl can be converted to another compound wherein R is H by reacting with aluminum chloride. The compound of formula II used as a starting material can be obtained by reacting a phenol, etc. with (perfluoroalkyl)aryl iodonium salt, and treating the reaction product with a base in the presence of acetocyanhydrin.
      COPYRIGHT: (C)1984,JPO&Japio
    • 新材料:式Ⅰ化合物(Rf为低级全氟烷基; R为H或叔烷基)。 实施例:4-(1'-氰基-2' ,2' ,2'-三氟乙基)-2,6-二叔丁基苯酚。 用途:对羟基苯基-α-三氟甲基 - 乙酸或其酯可用作头孢菌素修饰剂的合成中间体。 方法:式I化合物可以通过在还原催化剂(例如Pd / C)的存在下催化氢化式II的醌化合物来制备。 该反应优选在0-60℃的溶剂(例如乙腈)中进行。 其中R是叔烷基的式I化合物可以通过与氯化铝反应转化为其中R为H的另一化合物。 用作原料的式II化合物可以通过使苯酚等与(全氟烷基)芳基碘鎓盐反应,并在乙酰甘油存在下用碱处理反应产物来获得。