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    신규의치환된이미다졸유도체및그의제조방법
    2.
    发明授权
    신규의치환된이미다졸유도체및그의제조방법 失效
    新的取代的咪唑衍生物及其制备方法

    公开(公告)号：KR100303944B1

    公开(公告)日：2001-11-22

    申请号：KR1019930026610

    申请日：1993-12-06

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  이규양 ,  이상희 ,  김혜령 ,  서지희 ,  김낙정 ,  김선주 ,  차옥자 ,  신영아 ,  신화섭 ,  이승호 ,  정이숙 ,  이병호 ,  서호원

    IPC: C07D403/10

    Abstract: PURPOSE: Provided are novel substituted imidazole derivatives, represented by the formula(1) and their pharmaceutically acceptable salts, a pharmaceutical composition containing them and their preparation method. The compounds are used in inhibiting the high blood pressure by inhibiting the action of Angiotensin II. CONSTITUTION: The imidazole derivatives are represented by the formula(1), wherein A and B are independently -CH2 or -CO- but not -CO- simultaneously; Z is halogen atom or trifluorophenyl, C1-C14 alkenyl group; R is X substituted phenyl or thiophenyl, furanyl and imidazoyl(where x is -(CH2)n-X' and n is an integer of 0-4), and X' is hydrogen, -N-(C1-C4 alkyl)2, C1-C4 alkyl N substituted or unsubstituted piperazine, 3-or 2-oxopiperazine, morpholine, piperidine, thiomorpholine or imidazole. The typical method of synthesis comprises the steps of: manufacturing 5-(4-((thiomorpholine-4-yl)methyl)-2-butyl-4-chloro-1-((2'-(1H- tetrazole-5-yl)bipheyl-4-yl)methyl)imidazole by dissolving 4-chlorobenzoic acid into benzene and adding thionylchloride, refluxing, concentrating and dissolving again in methylene chloride; adding this product to the methylene chloride solution of 2-butyl-4-chloro-5-(hydroxymethyl)-1-((2'-((1-ethoxyethyl)-1H-tetrazole-5-yl)biphenyl-4 -yl)methyl)imidazole and triethylamine; dissolving this compound in tetrahydrofuran(THF) and adding thiomorpholine and refluxing with heating for 20 hours and extracting with ethylacetate; and dissolving this compound in THF, adding 1N HCl, stirring at room temperature for 17 hours, neutralizing with 1N NaOH and extracting with ethyl acetate.

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