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    디아자비시클로아민 화합물과 그의 제조방법
    75.
    发明授权
    디아자비시클로아민 화합물과 그의 제조방법 失效
    二氮杂环胺化合物及其制备方法

    公开(公告)号：KR1019910009331B1

    公开(公告)日：1991-11-11

    申请号：KR1019890015204

    申请日：1989-10-23

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  박명환 ,  오종훈

    IPC: C07D487/04

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: Diazabicycloamine derivs. of formula (I) and their salts are new. In (I), m = 1-3; n = 1-2; and R1, R2 = H or lower alkyl. Also claimed is the preparation of (I) which comprises e.g. reacting tetrakis(halomethyl)ethylene (halo = Cl, Br or I) with NH3 to form (I) in which m and n = 1 and R1 and R2 = H. (I) is e.g. 3,7-diazabicyclo(3.3.0)oct-1(5)ene or 3,8-diazabicyclo(4.3.0)non-1(6)-ene. Cpd. (I) is used for mfg. new quinolone antibiotics (claimed), with high antibacterial activity against Gram negative and Gram positive bacteria and improved antibacterial activity against methicillin resistant Staphylococcus aureus compared to ofloxacin, norfloxacin and ciprofloxacin. The quinolone are used for treating urethritis. (I) is also used for the prepn. of cephalosporins. cpds.

    Abstract translation: 二氮杂双环胺衍生物。 的式（I）及其盐是新的。 在（I）中，m = 1-3; n = 1-2; 和R 1，R 2 = H或低级烷基。 还要求保护的是（I）的制备，其包括例如 使四（卤代甲基）乙烯（卤代= Cl，Br或I）与NH 3反应形成其中m和n = 1且R 1和R 2 = H的（I）。 3,3-二氮杂双环（3.3.0）辛-1（5）烯或3,8-二氮杂双环（4.3.0）非-1（6）烯。 CPD。 （I）用于制造。 与氧氟沙星，诺氟沙星和环丙沙星相比，新型喹诺酮类抗生素（要求保护）对革兰氏阴性和革兰氏阳性菌具有较高的抗菌活性，对耐甲氧西林金黄色葡萄球菌的抗菌活性更好。 喹诺酮用于治疗尿道炎。 （I）也用于制备。 的头孢菌素。 国家方案文件。

    항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
    76.
    发明授权
    항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법 失效
    抗微生物喹啉化合物及其制备方法

    公开(公告)号：KR1019910009330B1

    公开(公告)日：1991-11-11

    申请号：KR1019890015202

    申请日：1989-10-23

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  박명환 ,  오종훈 ,  정명희 ,  김봉진

    IPC: C07D487/04

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: Quinolone derivs. of formula (I) and their acid addn. salts are new. In (I), X = C-H, C-F N; Z = H, halo or NH2; R1 = H or a cation; R2 = C1-4 (halo)hlkyl or hydroxyalkyl, or vinyl, C3-6 cycloalkyl or fluorophenyl; R3 = H, lower alkyl or formyl; m = 1- 3; n = 1 or 2. Also claimed is preparation of (I) which comprises e.g. condensing the corresponding quinolone derivative having a leaving gp. in the 7-position with a diazabicycloamine. (I) have improved and wider range of antibacterial activity against Gram positive and Gram negative bacteria than existing quinolone antibacterial agents, esp. norfloxacin, ciprofloxacin and ofloxacin. (I) have good antibacterial activity against methicillin resistant bacteria.

    Abstract translation: 喹诺酮衍生物。 的式（I）和它们的酸加成。 盐是新的。 在（I）中，X = C-H，C-F N; Z = H，卤素或NH 2; R1 = H或阳离子; R2 = C1-4（卤代）烷基或羟基烷基，或乙烯基，C3-6环烷基或氟苯基; R3 = H，低级烷基或甲酰基; m = 1- 3; n = 1或2.还要求保护的是（I）的制备。 冷凝具有离去gp的相应喹诺酮衍生物。 在7-位与二氮杂双环胺。 （I）比现有的喹诺酮类抗菌药物具有改善和更广泛的抗革兰氏阳性和革兰氏阴性菌的抗菌活性。 诺氟沙星，环丙沙星和氧氟沙星。 （I）对耐甲氧西林细菌具有良好的抗菌活性。

    3-피롤린 유도체와 그의 제조방법
    78.
    发明授权
    3-피롤린 유도체와 그의 제조방법 失效
    3-吡咯啉衍生物及其制备

    公开(公告)号：KR1019910002154B1

    公开(公告)日：1991-04-06

    申请号：KR1019890003658

    申请日：1989-03-23

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  이태석 ,  남근수 ,  김봉진

    IPC: C07D207/22 ,  C07D207/20

    Abstract: 3-Pyrroline derivs. of formula (I) comprises (a) cyclization condensation reaction of ethyl-N-benzyl-N-(beta-carboxyethyl) glynate of formula (II) and sodium ethoxide to produce keto-form 1- benzyl-3-carboethoxy-4-pyrrolidone (IV), (b) reducing, acetylating (IV), and adding anhydrous potassium carbonate to produce 1-benzyl-3-carboethoxy-3-pyrroline (V), (c) selective reduction of ester gp. of (V) to hydroxy gp. to produce 1- benzyl-3-hydroxymethyl-3-pyrroline (III), and (d) removing the benzyl gp. of (III) with alkoxychloroformate and reacting the resulting cpd. with R1R2NH. (I) have antibacterial activity.

    Abstract translation: 3-吡咯啉衍生物。 式（I）的化合物包括（a）式（II）的乙基-N-苄基-N-（β-羧乙基）甘氨酸和乙醇钠的环化缩合反应，生成酮型1-苄基-3-乙氧羰基-4- 吡咯烷酮（IV），（b）还原，乙酰化（IV）和加入无水碳酸钾以产生1-苄基-3-乙氧羰基-3-吡咯啉（V），（c）选择性还原酯gp。 （V）至羟基gp。 制备1-苄基-3-羟甲基-3-吡咯啉（III），和（d）除去苄基gp。 （III）与氯代甲酸烷基酯反应，并使所得的cpd反应。 与R1R2NH。 （I）具有抗菌活性。

    신규한 3-아자비시클로[3.1.1]헵탄 유도체 및 그의 제조방법
    80.
    发明授权
    신규한 3-아자비시클로[3.1.1]헵탄 유도체 및 그의 제조방법 失效
    新颖的3-AZABICYCLO£3,1,1 | HEPTANE衍生物及其制备方法

    公开(公告)号：KR1019970005303B1

    公开(公告)日：1997-04-15

    申请号：KR1019930023509

    申请日：1993-11-06

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  박태호 ,  김문환

    IPC: C07D471/08 ,  C07D295/00

    CPC classification number: Y02P20/55

    Abstract: The invention provides 3-azabicyclo[3.1.3 heptane derivatives which are useful for preparation of novel quinolone and beta-lactam antibiotics and a process for producing said derivatives. These derivatives are represented by the formula (I) wherein; n is 0 or 1; each R1, R2 and R3 is hydrogen, low alkyly or amino protecting group such as benzyl and low alcoxycarbonyl; R4 is hydrogen, unsubstituted low alkyl group, or low alkyl group substituted by hydroxy, amino group, low alcoxy group, low alkylamino group or halogen.

    Abstract translation: 本发明提供了可用于制备新型喹诺酮和β-内酰胺抗生素的3-氮杂双环[3.1.3庚烷衍生物及其制备方法。 这些衍生物由式（I）表示，其中： n为0或1; 每个R 1，R 2和R 3是氢，低烷基或氨基保护基如苄基和低烷氧基羰基; R4是氢，未取代的低级烷基或被羟基，氨基，低烷氧基，低级烷基氨基或卤素取代的低级烷基。

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