首页> 外国专利> Condensed pyrimidine derivatives with a on the pyrimidine ring fused, ring having a sulfur atom, a process for their preparation and pharmaceutical compositions containing same, as well as 2 - (halogen alkylene thio) - or 2 - (halogen vinylene thio) - 4,6 - di - (amino) - pyrimidines and process for the preparation of the latter

Condensed pyrimidine derivatives with a on the pyrimidine ring fused, ring having a sulfur atom, a process for their preparation and pharmaceutical compositions containing same, as well as 2 - (halogen alkylene thio) - or 2 - (halogen vinylene thio) - 4,6 - di - (amino) - pyrimidines and process for the preparation of the latter

机译:在嘧啶环上稠合的,具有硫原子的环上稠合的嘧啶衍生物,其制备方法和药物组合物,以及含有2-(卤代亚烷基硫基)-或2-(卤代亚乙烯基硫基)-4的药物组合物, 6-二-(氨基)-嘧啶类及其制备方法

摘要

The compounds of the general formula I IMAGE (I) and pharmaceutically acceptable acid addition salts and hydrates thereof possess useful immunostimulant properties and can be used in therapy. In the general Formula I A stands for -CH2-CH2-, -CH2-CH2-CH2-, -CH2-CH2-CH2CH2-or -CH=CH-; R4 is hydrogen, C1-4 alkyl or optionally substituted phenyl; r is 0, 1, 2, 3 or 4; R1 stands for hydrogen of C1-5 alkanoyl; R2 represents hydrogen, C1-5 alkanoyl or a group of the general formula (a) IMAGE (a) wherein R stands for hydrogen, C1-4 alkyl, C2-4 alkenyl, phenyl or phenyl-C1-3 alkyl and R3 stands for hydrogen. The compounds of the general Formula I can be prepared by reacting a 2-mercapto-4,6-diamino-pyrimidine of the general Formula II IMAGE (II) with a dihalo compound of the general Formula III IMAGE (III) (wherein Y and Z are halogen).
机译:通式I (I)的化合物及其药学上可接受的酸加成盐和水合物具有有用的免疫刺激特性,可用于治疗。在通式IA中,A代表-CH 2 -CH 2-,-CH 2 -CH 2 -CH 2-,-CH 2 -CH 2 -CH 2 CH 2-或-CH = CH-。 R4为氢,C1-4烷基或任选取代的苯基; r是0、1、2、3或4; R 1代表C 1-5烷酰基的氢; R 2代表氢,C 1-5烷酰基或通式(a)的基团[IMAGE](a)其中R代表氢,C 1-4烷基,C 2-4烯基,苯基或苯基-C 1-3烷基和R 3代表氢。通式I的化合物可以通过使通式II (II)的2-巯基-4,6-二氨基-嘧啶与通式III (III)的二卤代化合物反应来制备(其中Y和Z是卤素)。

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