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BICYCLIC NITROGEN-CONTAINING DERIVATIVES OR THEIR SALTS WITH MINERAL AND ORGANIC ACIDS OR BASES, METHODS OF THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS
BICYCLIC NITROGEN-CONTAINING DERIVATIVES OR THEIR SALTS WITH MINERAL AND ORGANIC ACIDS OR BASES, METHODS OF THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS
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机译:含矿物质和有机酸或碱的双环含氮衍生物或其盐,其制备方法和根据其组成的药物成分
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FIELD: organic synthesis. SUBSTANCE: invention relates to high-efficiency angiotensin II receptor antagonists and provides compounds with general formula I: where R2B and R3B, the same or different, are hydrogen, lower alkyl, lower fluoroalkyl, and lower thioalkyl; A1B, A2B, A3B and A4B are carbon or nitrogen, one or two of them being nitrogen and at least one of them being methyne group; R3 is hydrogen, hydroxyl, alkyl, hydroxyalkyl, phenyl, alkoxycarbonyl, and thioalkyl; R4 hydrogen, hydroxyl, arylalkyl, arylalkoxy, aryloxy, and arylamino groups. Compound I is prepared by reaction of compound II (formula ) with compound where are the same as R2B and R3B in compound I, are R4 in which reactive groups can be protected, and alk is C1-C6-alkyl, to form compound III (formula ) that is further subjected to cyclization. Reaction is carried out in organic solvent. EFFECT: new efficient drugs prepared. 7 cl, 38 ex
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机译:领域:有机合成。物质:本发明涉及高效血管紧张素II受体拮抗剂,并提供具有通式I的化合物:其中R 2B Sub>和R 3B Sub>相同或不同的是氢,低级烷基,低级氟烷基和低级硫代烷基; A 1B Sub>,A 2B Sub>,A 3B Sub>和A 4B Sub>是碳或氮,其中一个或两个是碳氮,其中至少一个为亚甲基; R 3 Sub>是氢,羟基,烷基,羟烷基,苯基,烷氧羰基和硫代烷基; R 4 Sub>氢,羟基,芳基烷基,芳基烷氧基,芳氧基和芳基氨基。化合物I是通过化合物II(公式)与化合物其中<图像文件=” 00000007.GIF“ he =” 6“ imgContent =” undefined“ imgFormat =” GIF “ wi =” 22“ />与化合物I中的R 2B Sub>和R 3B Sub>相同,是R 4 Sub>,其中可保护反应性基团,而alk是C 1 Sub> -C 6 Sub>-烷基,形成进一步的化合物III(分子式)进行环化。反应在有机溶剂中进行。效果:制备了新的有效药物。 7 cl,前38
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