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    • 81. 发明专利
    • Benzoic acid derivative
    • 苯甲酸衍生物
    • JPS6122047A
    • 1986-01-30
    • JP14119484
    • 1984-07-07
    • Koichi Shiyudo
    • SHIYUDOU KOUICHI
    • C07D303/38A61K31/165A61K31/19A61K31/195A61K31/215A61K31/235A61K31/335A61K31/336A61K31/655A61P35/02C07C51/00C07C51/09C07C65/32C07C65/38C07C67/00C07C69/76C07C69/78C07C233/65C07C233/78C07C233/81C07C241/00C07C245/08C07C291/08C07D303/40
    • NEW MATERIAL:The benzoic acid derivative of formula I (R
      1 and R
      2 are H, lower or medium alkyl or together form a 5W6-membered cycloalkyl, at least one of R
      1 and R
      2 is not H; R
      3 is OH, lower alkoxy or -NR
      4 R
      5 ; R
      4 and R
      5 are H or lower alyl; X is group of formula II, formula III, -N=N-, etc.; R
      6 and R
      7 are H or lower alkyl).
      USE: It has the activity to morphologically and functionally promote the differentiation of cancer cell, especially leukemia cell, and is useful as a drug.
      PREPARATION: The objective compound of formula I can be prepared by condensing the compound of formula I wherein X is -CO-C(R
      6 )=CH- with corresponding acetophenone derivative and a terephthalaldehydic acid ester or its derivative in the presence of a base. As an alternative method, the objective compound wherein the group X is formula III is produced by oxidizing a compound wherein the corresponding group X is C(R
      6 )=C(R
      7 ) with an epoxidizing agent.
      COPYRIGHT: (C)1986,JPO&Japio
    • 新物质:式I的苯甲酸衍生物(R1和R2是H,低级或中性烷基或一起形成5-6元环烷基,R 1和R 2中的至少一个不是H; R 3是OH,低级烷氧基或 -NR4R5; R4和R5是H或低级烯丙基; X是式II,式III,-N = N-等基团; R6和R7是H或低级烷基)。 用途:具有形态和功能促进癌细胞特别是白血病细胞分化的活性,可用作药物。 制备:式I的目标化合物可以通过在碱的存在下将其中X为-CO-C(R 6)= CH-的式I化合物与相应的苯乙酮衍生物和对苯二甲酸酯或其衍生物缩合而制备。 作为替代方法,其中基团X是式III的目标化合物是通过用环氧化剂氧化相应的基团X为C(R 6)= C(R 7)的化合物而制备的。