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1.发明公开
公开(公告)号：KR1020020002461A
公开(公告)日：2002-01-09
申请号：KR1020017014647
申请日：2000-05-18
Applicant: 동화약품주식회사
IPC: C07D471/04
CPC classification number: C07D401/04 , C07D471/04 , C07D487/10
Abstract: PURPOSE: Provided are optically active quinoline carboxylic acid derivatives, pharmaceutically acceptable salts thereof, solvates thereof, and a process for preparation thereof, which are useful for an antibacterial agent. CONSTITUTION: The optically active quinoline carboxylic acid derivatives are represented by the following formula(1), and contains optical activity-causing 4-aminomethyl-4-methyl-3 (Z)-alkoxyiminopyrrolidine substituents at the 7-position of the quinolone nuclei, their pharmaceutically acceptable salts, and their solvates. In the formula(1), Q is C-H, C-F, C-Cl or N; Y is H or NH2; R is a straight or branched alkyl group of Cl-C, an allyl group or a benzyl group, and * represents optically pure chiral carbon atom. Their preparation process comprises the steps of: condensing the quinolone nuclei-containing compound of formula(3), with the ketal compound of formula(2a), in the presence of an acid acceptor to give the optically active quinoline carboxylic acid derivative of formula(4); deketalizing the optically active quinoline carboxylic acid derivative of formula(4) to give the pyrrolidinone compound of formula(5); and reacting the pyrrolidinone compound of formula(5) with an alkoxylamine in the presence of a base to obtain the desired compound of formula(1).
Abstract translation: 目的：提供可用于抗菌剂的光学活性喹啉羧酸衍生物，其药学上可接受的盐，溶剂合物及其制备方法。 构成：光学活性喹啉羧酸衍生物由下式（1）表示，并且在喹诺酮核的7-位含有光学活性的4-氨基甲基-4-甲基-3（Z） - 烷氧基亚氨基吡咯烷取代基， 其药学上可接受的盐及其溶剂合物。 在式（1）中，Q是C-H，C-F，C-Cl或N; Y为H或NH 2; R是Cl-C，烯丙基或苄基的直链或支链烷基，*表示光学上纯的手性碳原子。 它们的制备方法包括以下步骤：在酸受体存在下将式（3）的喹诺酮核含有化合物与式（2a）的缩酮化合物缩合，得到式（3）的光学活性喹啉羧酸衍生物 4）; 对式（4）的光学活性喹啉羧酸衍生物进行缩酮化，得到式（5）的吡咯烷酮化合物; 并在碱的存在下使式（5）的吡咯烷酮化合物与烷氧基胺反应，得到所需的式（1）化合物。
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2.发明授权
公开(公告)号：KR100497942B1
公开(公告)日：2005-06-29
申请号：KR1020017014647
申请日：2000-05-18
Applicant: 동화약품주식회사
IPC: C07D471/04
CPC classification number: C07D401/04 , C07D471/04 , C07D487/10
Abstract: 본 발명은 광학활성의 퀴놀린 카르복실산 유도체, 이의 약학적으로 허용되는 염, 이의 용매화물 및 이의 제조방법에 관한 것으로, 구체적으로 본 발명은 퀴놀론 모핵의 7-위치에 광학활성을 유발하는 4-아미노메틸-4-메틸-3-(Z)-알콕시이미노피롤리딘 치환체를 갖는 광학활성의 퀴놀린 카르복실산 유도체에 관한 것으로, 본 발명의 화합물은 그의 거울상 이성질체, 라세믹 혼합물 및 기존의 항균제에 비하여 항균 효과가 매우 우수하고 약동력학적 특성이 우수할 뿐만 아니라 광독성도 거의 나타내지 않기 때문에 항균제로서 효과적으로 사용될 수 있다.
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3.发明公开
公开(公告)号：KR1020010029698A
公开(公告)日：2001-04-06
申请号：KR1020000024657
申请日：2000-05-09
Applicant: 동화약품주식회사
IPC: C07D403/04
Abstract: PURPOSE: Provided is a method for manufacturing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative which has antibacterial effects on both gram positive and negative bacteria so that the derivative is useful for medical purposes. And Its pharmaceutically acceptable salt and its solvate are also provided. CONSTITUTION: A method for producing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative comprises the following steps of: i) reacting the compound of the formula (3) with ketal compound of the formula (2a) in the presence of acid receptor, for 1-24 hours at 0-150 deg.C, preferably from room temperature to 90 deg.C, to manufacture optically active quinoline carboxylic acid derivative of the formula (4); ii) deketalizing the quinoline carboxylic acid derivative to manufacture pyrrolidinone of the formula (5) at from room temperature to 100 deg.C; and iii) reacting the pyrrolidinone with alkoxylamine in the presence of base at 0-90 deg.C. In the formula (1), Q is C-H, C-F, C-CL, or N. Y is H or NH2. R is a C1-C4 linear or branched alkyl, aryl, or benzyl group. * is an optically pure asymmetric carbon.
Abstract translation: 目的：提供对革兰氏阳性细菌和阴性细菌都具有抗菌作用的4-氨基甲基-4-甲基-3-（Z） - 烷氧基氨基衍生物的制备方法，因此该衍生物可用于医疗目的。 还提供其药学上可接受的盐及其溶剂合物。 构成：4-氨基甲基-4-甲基-3-（Z） - 烷氧基氨基衍生物的制备方法包括以下步骤：i）使式（3）的化合物与式（2a）的缩酮化合物反应于 存在酸受体，在0-150℃，优选室温至90℃下进行1-24小时，以制备式（4）的光学活性喹啉羧酸衍生物; ii）将喹啉羧酸衍生物缩酮化，制备式（5）的吡咯烷酮，室温至100℃; 和iii）在0-90℃下，在碱的存在下使吡咯烷酮与烷氧基胺反应。 在式（1）中，Q是C-H，C-F，C-CL或N.Y是H或NH 2。 R是C1-C4直链或支链烷基，芳基或苄基。 *是光学纯的不对称碳。
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