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    스피로알킬아민 유도체와 그의 제조방법
    31.
    发明授权
    스피로알킬아민 유도체와 그의 제조방법 失效
    螺甲基胺衍生物

    公开(公告)号：KR1019960011370B1

    公开(公告)日：1996-08-22

    申请号：KR1019910025885

    申请日：1991-12-31

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  박명환 ,  하재두 ,  백경업

    IPC: C07D209/12

    CPC classification number: C07D221/20 ,  C07D209/54 ,  Y02P20/55

    Abstract: Spiroalkylamine derivatives and their salts have a general formula (I), wherein R1 is hydrogen, substituted or unsubstituted C1-C20 alkyl, substituted or unsubstituted benzyl, formyl, substituted or unsubstituted C1-C5 alkylcarbonyl, substituted or unsubstituted benzoyl, substituted or unsubstituted C1-C5 alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, substituted or unsubstituted C1-C5 alkylsulfonyl, or substituted or unsubstituted benzenesulfonyl; R2 is hydrogen or methyl substituted at the position of 4 or 6; R3 is hydroxy, hydroxymethyl, carboxy, C1-C4 alkoxy, C2-C5 alkoxymethyl, C2-C5 acyloxy, C3-C6 acyloxymethyl, methanesulfonyloxy, methanesulfonyloxymethyl, p-toluenesulfonyloxy, p-toluenesulfonyloxymethyl, cyanato, C2-C6 alkoxycarbonyl, azidocarbonyl, C1-C8 alkyl, C1-C5 alkoxycarbonyl, aminocarbonyl substituted or unsubstituted benzyl or -(CH2)m-NR4R5, where m is 0 or 1; R4 is hydrogen, C1-C4 alkanoyl or benzoyl; and R5 is hydrogen, C1-C4 -alkyl, nitrogen protective group degradable in a living body, n is 1 or 2, diastereomers may be (1,3)-R,S, (1,3)-R,R, (1,3)-S,S or (1,3)-S,R.

    Abstract translation: 螺烷基胺衍生物及其盐具有通式（I），其中R1是氢，取代或未取代的C1-C20烷基，取代或未取代的苄基，甲酰基，取代或未取代的C1-C5烷基羰基，取代或未取代的苯甲酰基，取代或未取代的C1 C 5烷氧基羰基，取代或未取代的苄氧基羰基，取代或未取代的C 1 -C 5烷基磺酰基，或取代或未取代的苯磺酰基; R2为4或6位的氢或甲基取代; R3是羟基，羟甲基，羧基，C1-C4烷氧基，C2-C5烷氧基甲基，C2-C5酰氧基，C3-C6酰氧基甲基，甲磺酰氧基，甲磺酰氧基甲基，对甲苯磺酰氧基，对甲苯磺酰氧基甲基，氰基，C2-C6烷氧羰基，叠氮羰基，C1 C 1-8烷基，C 1 -C 5烷氧基羰基，氨基羰基取代或未取代的苄基或 - （CH 2）m -NR 4 R 5，其中m为0或1; R4是氢，C1-C4烷酰基或苯甲酰基; R5为氢，C1-C4烷基，可在生物体中降解的氮保护基，n为1或2，非对映异构体可为（1,3）-R，S，（1,3）-R，R（（ 1,3）-S，S或（1,3）-S，R。

    신규 퀴놀론 화합물
    34.
    发明授权
    신규 퀴놀론 화합물 失效
    新的喹诺酮类化合物

    公开(公告)号：KR1019940002955B1

    公开(公告)日：1994-04-09

    申请号：KR1019910006363

    申请日：1991-04-20

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  박명환 ,  하재두 ,  백경업

    IPC: C07D487/04

    Abstract: The quinolone cpd. or its salts of formula (I) are prepd. by heating and reacting the cpd. (II) with the cpd. (III) or (IIIa) in presence of the base. In the formulas, R1 is opt. substd. C1-7 lower alkyl, opt. substd. C3-7 cycloalkyl, opt. substd. lower alkenyl, opt. substd. phenyl; R2 is H, protecting gp. of carboxyl gp. or pharmaceutically usuable metalic or organic cation; R3 is H or C1-4 lower alkyl, C2-4 hydroxy alkyl, C3-7 cycloalkyl or biodegradable N-protecting gp.; X is Cl or Br; Z is methyl; n is 1-3; n is 1 or 2; A is Cl or Br; L is halogen, ethane sulfonyl or paratoluene sulfonyl. The compound is antibacterial.

    Abstract translation: 喹诺酮cpd 或其式（I）的盐是制备的。 通过加热和反应cpd。 （II）与cpd。 （III）或（IIIa）。 在公式中，R1是opt。 substd。 C1-7低级烷基，选择。 substd。 C3-7环烷基， substd。 低级链烯基 substd。 苯基; R2是H，保护gp。 的羧基gp。 或药学上可用的金​​属或有机阳离子; R3是H或C1-4低级烷基，C2-4羟基烷基，C3-7环烷基或可生物降解的N-保护性gp。 X是Cl或Br; Z是甲基; n为1-3; n为1或2; A是Cl或Br; L是卤素，乙磺酰基或对甲苯磺酰基。 该化合物是抗菌的。

    신규한 퀴놀론화합물과 그 제조방법
    35.
    发明授权
    신규한 퀴놀론화합물과 그 제조방법 失效
    新型喹啉酮化合物及其制备方法

    公开(公告)号：KR1019930006164B1

    公开(公告)日：1993-07-08

    申请号：KR1019910001726

    申请日：1991-02-01

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  박명환 ,  백경업 ,  이태석 ,  남근수

    IPC: C07D487/04

    Abstract: Quninolone derivs. of formula (I) and their salts are new. In (I), R1=H, carboxyl protecting gp., Na or K; R2=C1-6 alkyl, halogenated alkyl, alkenyl, C3-6 cycloalkyl, (halogenated) phenyl or X-O(or S)-CH2CH(CH3)-N-; Z=H, halogen or amino; R3=Cl, Br or F; X=N or C-Y; Y=H, F, Cl, Br or CH3; R4= cycloalkyl, hydroxy, hydroxyalkyl, amino or biode-gradable nitrogen protecting gp.; m = 1- 3; n = 1-2. Also claimed is the prepen. of (I) which comprises a condensation reaction of a cpd. of formula (II) with a cpd. of formula (III) in a solvent in the presence of a base at 15-200 deg.C. The cpds. (I) have a good antibacterial activity.

    Abstract translation: Quninolone衍生物。 的式（I）及其盐是新的。 在（I）中，R 1 = H，羧基保护基，Na或K; R 2 = C 1-6烷基，卤代烷基，烯基，C 3-6环烷基，（卤代）苯基或X-O（或S）-CH 2 CH（CH 3） Z = H，卤素或氨基; R3 = Cl，Br或F; X = N或C-Y; Y = H，F，Cl，Br或CH 3; R4 =环烷基，羟基，羟基烷基，氨基或生物降解氮保护gp。 m = 1- 3; n = 1-2。 还声称是prepen。 的（I），其包含cpd的缩合反应。 的式（II）与cpd。 式（III）的化合物在溶剂中，在碱存在下，在15-200℃。 cpds。 （I）具有良好的抗菌活性。

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