首页> 外国专利> SELECTIVE PROTIVOTUBERKULEZYNE agent are asymmetrically 3,6-disubstituted 1,2,4,5-tetrazine AND METHOD FOR THEIR PREPARATION

SELECTIVE PROTIVOTUBERKULEZYNE agent are asymmetrically 3,6-disubstituted 1,2,4,5-tetrazine AND METHOD FOR THEIR PREPARATION

机译:3,6-二取代的1,2,4,5-四嗪不对称选择的PROVOVOTUBERKULEZYNE试剂及其制备方法

摘要

1. Selective antituberculosis agents, which are 3-substituted amino-6- (3,5-dimethylpyrazole-1-yl) -1,2,4,5-tetrazine of formula R = amino Agde, CC--alkyl, 3-hydroxy -5-hydroxypentyl, propyn-2-yl, ethylindole, adamantyl, aryl selected from optionally substituted phenyl, heteryl selected from quinolin-3-yl, pyridyl, phenyl substituted with a substituent selected from the group consisting of methyl, chloro , methoxy, and pyridyl is substituted with substituents selected from chloro, metil.2. Selective antituberculosis agents, which are 3-substituted hydrazino-6- (3,5-dimethylpyrazole-1-yl) -1,2,4,5-tetrazine of formula B or BR = a hydrogen atom or methyl; R = methyl, 1-phenylpropen-1-yl, aryl selected from optionally substituted phenyl, heteryl selected from furyl, pyridyl, wherein the phenyl is substituted with 1-3 substituents selected from the group consisting of bromo, chloro, methoxy, nitro, , a hydroxy group, n = 0, 1, 2.3. A method for producing 3-gidrazinozameschennyh 6- (3,5-dimethylpyrazole-1-yl) -1,2,4,5-tetrazine of formula B or C according to claim 2, which comprises reacting equimolar amounts of 3-hydrazino-6- (3 5-dimethylpyrazole-1-yl) -1,2,4,5-tetrazine and aryl, getarilaldegida, aromatic or aliphatic ketone under heating in an organic solvent, characterized in that the process is carried out under the effect of 200 watt microwave irradiation at a temperature of 55-60 ° C for 15-20 min, and in acetonitrile is used as the organic solvent.
机译:1.选择性抗结核药,它们是式3取代的氨基6-(3,5-二甲基吡唑-1-基)-1,2,4,5-四嗪R =氨基阿格德,CC-烷基,3-羟基-5-羟基戊基,丙-2-基,乙基吲哚,金刚烷基,选自任选取代的苯基的芳基,选自喹啉-3-基的杂基,吡啶基,被选自甲基,氯,甲氧基的取代基取代的苯基,吡啶基被选自氯,甲氧基2的取代基取代。选择性抗结核药,是式B或BR的3-取代的肼基-6-(3,5-二甲基吡唑-1-基)-1,2,4,5-四嗪=氢原子或甲基; R =甲基,1-苯基丙烯-1-基,选自任选取代的苯基的芳基,选自呋喃基,吡啶基的杂基,其中苯基被1-3个选自溴,氯,甲氧基,硝基的取代基取代,羟基,n = 0、1、2.3。 3.根据权利要求2所述的制备式B或C的3-gidrazinozameschennyh 6-(3,5-二甲基吡唑-1-基)-1,2,4,5-四嗪的方法,其包括使等摩尔量的3-肼基-在有机溶剂中加热下,使6-(3 5二甲基吡唑-1-基)-1,2,4,5-四嗪和芳基,芳基萘,芳族或脂族酮,其特征在于,该方法在以下条件下进行: 200瓦微波在55-60°C的温度下照射15-20分钟,并在乙腈中用作有机溶剂。

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