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    이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법
    21.
    发明公开
    이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법 有权
    由含有咪唑的二级胺取代的苯并噻吩衍生物及其制备方法

    公开(公告)号：KR1020040014023A

    公开(公告)日：2004-02-14

    申请号：KR1020020047189

    申请日：2002-08-09

    Applicant: 한국화학연구원

    Inventor： 이규양 ,  이선경 ,  유성은 ,  서지희 ,  김낙정 ,  황선경 ,  김은숙 ,  이병호 ,  서호원 ,  이정옥 ,  최상운

    IPC: C07D405/12

    CPC classification number: C07D405/12

    Abstract: PURPOSE: Benzopyran derivatives substituted by secondary amine containing imidazole and a method for preparing the same are provided. The compounds are useful for treatment of cancer, diabetic retinopathy and external brain wound. CONSTITUTION: Benzopyran derivatives substituted by secondary amine containing imidazole represented by the formula(1), partial stereo isomers thereof and pharmaceutically acceptable salts thereof are provided, wherein R1 is H, CN, NO2 or NH2; R2 is CH3, CHORaRa or CHOOZ; Ra is C1-C4 linear or branched chain alkyl; Z is C2-C6 linear or branched chain alkyl; R3 and R4 are independently H, Cl, Br, F, C1-C3 linear or branched chain alkyl, ORb, CF3, OCF3, NO2 or CO2Rb; Rb is H or C1-C3 alkyl; and * is chiral carbon. A method for preparing the compound of the formula(I) comprises reacting epoxide compounds of the formula(II) with imidazole containing secondary amine compounds of the formula(III) in the presence of metal salt and a solvent, wherein the metal salt is selected from Mg(ClO4)2, COCl2, LiClO4, NaClO4, CaCl2, ZnCl2, LiBF4 and Zn(Tf)2; and the solvent is selected from acetonitrile, tetrahydrofuran and dimethylformamide.

    Abstract translation: 目的：提供由含仲胺的咪唑取代的苯并吡喃衍生物及其制备方法。 该化合物可用于治疗癌症，糖尿病性视网膜病变和外部脑部伤口。 构成：提供由式（1）表示的含仲胺的咪唑取代的苯并吡喃衍生物，其部分立体异构体及其药学上可接受的盐，其中R1为H，CN，NO2或NH2; R2是CH3，CHORaRa或CHOOZ; Ra是C1-C4直链或支链烷基; Z是C 2 -C 6直链或支链烷基; R 3和R 4独立地为H，Cl，Br，F，C 1 -C 3直链或支链烷基，ORb，CF 3，OCF 3，NO 2或CO 2 R b; Rb是H或C 1 -C 3烷基; 和*是手性碳。 制备式（I）化合物的方法包括在金属盐和溶剂的存在下使式（II）的环氧化合物与含有式（III）的仲胺化合物的咪唑反应，其中选择金属盐 从Mg（ClO4）2，COCl2，LiClO4，NaClO4，CaCl2，ZnCl2，LiBF4和Zn（Tf）2; 溶剂选自乙腈，四氢呋喃和二甲基甲酰胺。

    신규의치환된이미다졸유도체및그의제조방법
    22.
    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.

    벤조피란 유도체의 제조 방법
    26.
    发明授权
    벤조피란 유도체의 제조 방법 失效
    制备苯并吡喃衍生物的方法

    公开(公告)号：KR1019950009864B1

    公开(公告)日：1995-08-29

    申请号：KR1019910024354

    申请日：1991-12-26

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  정낙철 ,  서지희 ,  김선주

    IPC: C07D405/04

    Abstract: The cpd. of formula (I-a) is prepd. by (a) reacting ketone derivatives of formula (II) with trifluorosulfonic acid anhydride and ter-amine, or making the ketone derivatives (II) to enolate with a base and then reacting N-phenyl trifluoromethane sulfonimide to convert to the vinyl triflate derivs. of formula (III); and (b) reacting the derivs. (III) with pyridyl trialkyline derivs. of formula (IV) in the presence of palladium catalyst and chloride. In the formulas, R1 is -CN, -NO2, -OCX1X2X3, -NH2, -NHSO2Ra etc; X1, X2, and X3 are F, Cl or H; R3 is H or C1-6 alkyl or phenyl; R4 is C1-4 alkyl.

    Abstract translation: cpd。 的式（I-a）是制备的。 通过（a）使式（II）的酮衍生物与三氟磺酸酐和三胺反应，或使酮衍生物（II）与碱烯醇化，然后使N-苯基三氟甲磺酰亚胺反应转化成三氟甲磺酸乙烯酯衍生物。 的式（III）; 和（b）使衍生物反应。 （III）与吡啶基三烷基衍生物。 式（Ⅳ）化合物在钯催化剂和氯化物存在下反应。 式中，R1为-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2Ra等; X1，X2和X3分别为F，Cl或H; R3是H或C1-6烷基或苯基; R4是C1-4烷基。

    벤조피란 유도체와 그의 제조방법
    28.
    发明授权
    벤조피란 유도체와 그의 제조방법 失效
    新型苯并噻吩衍生物及其制备方法

    公开(公告)号：KR1019930011040B1

    公开(公告)日：1993-11-20

    申请号：KR1019900019034

    申请日：1990-11-23

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  이규양 ,  서지희 ,  신화섭 ,  이병호

    IPC: C07D405/04

    Abstract: Novel benzopyran derivatives of formula (I) are prepared by O- nitration at C-3 hydroxy group of cromakalim of formula (II) in the anhydride acetic acid or C.H2SO4. In the formula (I), R1 R2=H, NO2, nitryl; R3= 2-oxo-1-pyrrolidinyl. Compound (I) are useful as antihypertensive and vasodilating agents.

    Abstract translation: 式（I）的新型苯并吡喃衍生物通过在酸酐乙酸或C.H 2 SO 4中通过式（II）的cromakalim的C-3羟基进行O-硝化来制备。 在式（I）中，R1R2 = H，NO2，硝基; R3 = 2-氧代-1-吡咯烷基。 化合物（I）可用作抗高血压药和血管舒张剂。

    인단 유도체와 그의 제조방법
    29.
    发明授权
    인단 유도체와 그의 제조방법 失效
    制备印度衍生物的方法

    公开(公告)号：KR1019930006765B1

    公开(公告)日：1993-07-23

    申请号：KR1019910001326

    申请日：1991-01-26

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  서지희 ,  이규양 ,  신화섭 ,  이병호 ,  서호원

    IPC: C07D207/26 ,  C07D207/24

    Abstract: Indane derivs. of formula (I) are new. In (I), R1= nitro, nitrile, halogen, amino, CF3, -(C=NH)-OMe, -NHCOCS3, -NHCSCX3, - COR4, -OCX3 OR -CSR4; X=H or halogen; R4=H, amino, lower alkyl or alkoxy, or opt. substd. phenyl; R2=-NO5R6, a gp. of formula (II), a gp. of formula (III), a gp. of formula (IV), etc.; R5 and R6 each=H, lower alkyl, cyclopropyl, cyclopropyl methyl or benzyl; n = 1 or 2; Y=CH2, O, S or -NR4; R3=H, OH, nitrooxy, formyloxy, alkanoyloxy, haloalkanoyloxy, alkoxycarbonyl, aroyloxy or carbamoyloxy. The cpds. (2) may be used in the treatment of hypertension.

    Abstract translation: indane派生。 式（I）的化合物是新的。 在（I）中，R1 =硝基，腈，卤素，氨基，CF3， - （C = NH）-OMe，-NHCOCS3，-NHCSCX3，-COR4，-OCX3或-CSR4; X = H或卤素; R4 = H，氨基，低级烷基或烷氧基，或选择。 substd。 苯基; R2 = -NO5R6，gp。 的式（II），gp。 的式（III），gp。 的式（IV）等; R5和R6各自为H，低级烷基，环丙基，环丙基甲基或苄基; n = 1或2; Y = CH 2，O，S或-NR 4; R3 = H，OH，硝基氧基，甲酰氧基，烷酰氧基，卤代烷酰氧基，烷氧基羰基，芳氧基或氨基甲酰氧基。 cpds。 （2）可用于治疗高血压。

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