4,5-diaminopyrimidine derivatives and a method for the preparation thereof
    2.
    发明授权
    4,5-diaminopyrimidine derivatives and a method for the preparation thereof 失效
    4,5-二氨基嘧啶衍生物及其制备方法

    公开(公告)号:US06172227B2

    公开(公告)日:2001-01-09

    申请号:US08931306

    申请日:1997-09-16

    IPC分类号: C07D40112

    摘要: Novel 4,5-diamino pyrimidine derivatives are described by the following general formula I: in which X is a direct bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenyl or phenyl C1-4 alkylene; Y is a direct bond or C1-2 alkyl, R1 is (i) 5-15 membered cyclic or fused heterocompound which includes one or two atoms selected from a group consisting of nitrogen, oxygen and sulfur and which is substituted with one or two substituents selected from a group consisting of hydrogen, halogen, nitro, hydroxy, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy, (ii) C4-10 carbocyclic compound or (iii) hydroxy C1-4 alkoxy, R2 is 5-15 membered cyclic or fused heterocompound which includes one or two nitrogen atoms and, optionally, one oxygen or sulfur atom, and which is substituted with one or two substituents selected from a group consisting of hydrogen, hydroxy, halogen, nitro, hydroxy C1-5 alkyl, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy; R3 is hydrogen, in which R4 and R5 are each independently selected from a group consisting of hydroxy, C1-6 alkyl, C3-7 cycloalkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen C2-6 alkenyl and C1-4alkoxy or R4 and R5 represent each independently in which R6 is selected from a group consisting of hydrogen, hydroxy, C1-6 alkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen, nitro and C1-4 alkoxy.

    摘要翻译: 新的4,5-二氨基嘧啶衍生物由以下通式I描述:其中X是直接键,C 1-4亚烷基,C 1-4亚烷基氧基,C 1-4烷氧基苯基或苯基C 1-4亚烷基; Y是直接键或C1-2烷基,R1是(i)5-15元环或稠合杂化合物,其包含一个或两个选自氮,氧和硫的原子,并被一个或两个取代基取代 选自氢,卤素,硝基,羟基,C 1-6烷基,C 3-6烯基和卤素C 1-4烷氧基,(ii)C 4-10碳环化合物或(iii)羟基C 1-4烷氧基,R 2为 5-15元环或稠合杂化合物,其包含一个或两个氮原子和任选的一个氧或硫原子,并被一个或两个选自氢,羟基,卤素,硝基,羟基C1 烷基,C 1-6烷基,C 3-6烯基和卤素C 1-4烷氧基; R 3是氢,其中R 4和R 5各自独立地选自羟基,C 1-6烷基,C 3-7环烷基,C 3-6烯基,卤素C 1-6烷基,卤素C 2-6烯基和C 1-4烷氧基 或R 4和R 5各自独立地表示,其中R 6选自氢,羟基,C 1-6烷基,C 3-6烯基,卤素C 1-6烷基,卤素,硝基和C 1-4烷氧基。