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1. 发明授权

KR100950699B1 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르유도체의 산부가염, 이의 제조방법 및 이를 포함하는 약학조성물 失效
标题翻译： 2-亚甲基甜菜碱 - 碳酰基-3-羧酸酯衍生物的添加剂，其制备方法和包含其的药物组合物
公开(公告)号：KR100950699B1
公开(公告)日：2010-03-31
申请号：KR1020080028691
申请日：2008-03-28
申请人： 국제약품 주식회사 , 한국화학연구원
发明人： 김봉진 , 송복주 , 최영로 , 이범수 , 서동근 , 정영철 , 김시민
IPC分类号： C07D487/04 , C07D403/12
CPC分类号： Y02A50/473
摘要： 본 발명은 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르 유도체의 산부가염, 이의 제조방법 및 이를 포함하는 약학 조성물을 제공한다. 상기 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르 유도체의 산부가염은 안정성이 우수한 결정형으로 얻어지며, 높은 경구흡수율을 나타낸다. 또한, 상기 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르 유도체의 산부가염의 활성 대사체는 그람 양성균 및 그람 음성균에 대하여 광범위한 항균 활성을 나타내며, MRSA (메티실린 내성균주) 및 QRS (퀴놀론 내성균주)에 대한 우수한 항균 활성을 나타낸다.
카바페넴

2. 发明授权

KR100367986B1 광학활성을 갖는 시아노부탄트리올 유도체 및 그의 제조방법 有权
标题翻译：具有光学活性的氰基丁三醇衍生物及其制备方法
公开(公告)号：KR100367986B1
公开(公告)日：2003-01-14
申请号：KR1020000015512
申请日：2000-03-27
申请人： 국제약품 주식회사
发明人： 최영로 , 김관수 , 김진환
IPC分类号： C07C255/11
CPC分类号： C07D307/33 , C07B2200/07 , C07C255/12 , C07D317/30 , C07H3/02
摘要： The present invention relates to an optically active (2S,3R)-4-cyanobutan-1,2,3-triol derivative, a process for preparing same, and a process for preparing 2-deoxy-L-ribose from same.
摘要翻译：本发明涉及光学活性的（2S，3R）-4-氰基丁烷-1,2,3-三醇衍生物，其制备方法以及由其制备2-脱氧-L-核糖的方法。

3. 发明授权

KR100445781B1 (Ｓ)-1-아세틸-2-피롤리딘카복스아미드의 제조방법 失效
标题翻译：（S）-1-아세틸-2-피롤리딘카복스아미드의제조방（
公开(公告)号：KR100445781B1
公开(公告)日：2004-08-25
申请号：KR1020000071824
申请日：2000-11-30
申请人： 국제약품 주식회사
发明人： 최영로 , 강재효 , 이대원 , 이형주
IPC分类号： C07D207/10
摘要： PURPOSE: A process for preparing (S)-1-acetyl-2-pyrolidine carboxamide, which is useful as an intermediate in synthesis of Levosulpiride, is provided, thereby preparing the subject compound simply in higher yield. CONSTITUTION: The process for preparing (S)-1-acetyl-2-pyrolidine carboxamide comprises the steps of: (a) reacting (S)-proline of formula(2) with acetic acid anhydride, or alternatively (b) reacting (S)-proline of formula(2) with acetic acid anhydride; reacting the reaction compound with acylhalide of formula(3) to prepare a compound of formula(4); and reacting the compound of formula(4) with alcoholic ammonia to prepare (S)-1-acetyl-2-pyrolidine carboxamide of formula(1), wherein X is halogen and R is methyl, ethoxy or t-butyl; the addition mole ratio of the compound of formula(2) and acetic acid anhydride is 1:1 to 1:5; and the acylation is carried out in the presence of base selected from triethylamine, pyridine and dimethylamine.
摘要翻译：目的：提供一种制备作为左旋舒必利合成中间体有用的（S）-1-乙酰基-2-吡咯烷甲酰胺的方法，由此仅以更高的收率制备本发明化合物。（S）-1-乙酰基-2-吡咯烷甲酰胺的制备方法包括以下步骤：（a）使式（2）的（S） - 脯氨酸与乙酸酐反应，或者（b）使（S）） - 式（2）的脯氨酸与乙酸酐反应; 使反应化合物与式（3）的酰卤反应以制备式（4）的化合物; （4）化合物与醇氨反应以制备式（1）的（S）-1-乙酰基-2-吡咯烷甲酰胺，其中X为卤素且R为甲基，乙氧基或叔丁基; 式（2）化合物与乙酸酐的加成摩尔比为1：1至1：5; 酰化反应在选自三乙胺，吡啶和二甲胺的碱存在下进行。

4. 发明公开

KR1020000002240A 2-[(2,6-디클로로페닐)아미노]페닐아세톡시아세트산의제조방법 失效
标题翻译：制备2 - [（2,6-二氯苯基）氨基]苯基氧基 - 丙酸的方法
公开(公告)号：KR1020000002240A
公开(公告)日：2000-01-15
申请号：KR1019980022890
申请日：1998-06-18
申请人： 국제약품 주식회사
发明人： 최영로 , 이대원 , 김태훈 , 김성태
IPC分类号： C07C229/34
CPC分类号： Y02P20/55
摘要： PURPOSE: Title compound is prepared which has an anti-inflammatory and an analgesic property. CONSTITUTION: Iodine and silylating agent such as hexamethyl disilazane, hexamethyl disiloxane, hexamethyl disilane, phenylseleno trimethylsilane, phenyltrimethylsilane, allyltrimethylsilane, 3,6-bis£trimethylsilyl|1,4-cyclohexadiene are activated in polar solvent, followed by the reaction with compound(3) having t-butyl protecting group to give the title compound. Thus, 8.24 g t-butyl2-£2,6-dichlorophenyl)amino|phenylacetoxyacetate is dissolved in 100 ml dichloromethane, followed by addition of 3.06 g iodine and 2.53 ml hexamethyldisilazane, and reacted for 2 hours to give 6.23 g 2-£(2,6-dichlorophenyl)- amino|phenylaectoxyacetic acid.
摘要翻译：目的：制备具有抗炎和止痛特性的标题化合物。构成：六甲基二硅氮烷，六甲基二硅氧烷，六甲基乙硅烷，苯基硒基三甲基硅烷，苯基三甲基硅烷，烯丙基三甲基硅烷，3,6-双三甲基甲硅烷基| 1,4-环己二烯的碘和甲硅烷基化剂在极性溶剂中活化，随后与化合物 3）具有叔丁基保护基，得到标题化合物。因此，将8.24g 2-（2,6-二氯苯基）氨基苯基乙酰氧基乙酸叔丁酯溶于100ml二氯甲烷中，然后加入3.06g碘和2.53ml六甲基二硅氮烷，反应2小时得到6.23g 2-（ 2,6-二氯苯基） - 氨基|苯基乙氧基乙酸。

5. 发明公开

KR1020010092864A 광학활성을 갖는 시아노부탄트리올 유도체 및 그의 제조방법 有权
标题翻译：具有光合作用的氰基丁胺衍生物及其制备方法
公开(公告)号：KR1020010092864A
公开(公告)日：2001-10-27
申请号：KR1020000015512
申请日：2000-03-27
申请人： 국제약품 주식회사
发明人： 최영로 , 김관수 , 김진환
IPC分类号： C07C255/11
CPC分类号： C07D307/33 , C07B2200/07 , C07C255/12 , C07D317/30 , C07H3/02
摘要： PURPOSE: A method for synthesizing novel (2S,3R)-4-cyanobutane-1,2,3-triol derivative for the application as a precursor to the manufacture process of 2-dioxy-L-ribose that is a composition unit of meso-DNA and enantio-DNA that are useful as antisense drugs. The present (2S,3R)-4-cyanobutane-1,2,3-triol is easily synthesized by introducing cyano groups into the structure of epoxy compounds, and this method differ from conventional methods in which n-butyl lithium is required to activate dithiane compounds that are produced as intermediate. CONSTITUTION: The synthesizing method comprises the steps of (i) introducing cyano groups such as potassium cyanide and sodium cyanide into the epoxy compounds (formula III) in methanol solvent of ambient temperature range wherein the amount of cyano group is 6 to 10 equivalent weight based on the equivalent weight of the epoxy compound; (ii) hydrolyzing the (2S,3R)-4-cyano butane-1,2,3-triol derivative (formula I) obtained from 1st step; and then (iii) reducing the resultant obtained from 2nd step in tetrahydrofuran solvent to synthesize 2-dioxy-L-ribose (formula III) wherein £(Sia)2BH| is used as reductant. In the formula (I), R and R' represent hydrogen or hydroxy protection group respectively, and the hydroxy protection group is selected from isopropylidene, cyclohexylidene, benzylidene and benzyl.
摘要翻译：目的用于合成新型（2S，3R）-4-氰基丁烷-1,2,3-三醇衍生物的方法，用于作为内消旋组成单位的2-二氧基-L-核糖的制备过程的前体 -DNA和对映体DNA，可用作反义药物。本发明的（2S，3R）-4-氰基丁烷-1,2,3-三醇通过将氰基引入环氧化合物的结构中容易合成，并且该方法不同于需要正丁基锂来活化的常规方法作为中间体生产的二噻烷化合物。构成：合成方法包括以下步骤：（i）在环境温度范围的甲醇溶剂中将氰基氰化物和氰化钠等氰基引入到环氧化合物（式III）中，其中氰基的量为6至10当量相当于环氧化合物的重量; （ii）水解由第1步获得的（2S，3R）-4-氰基丁烷-1,2,3-三醇衍生物（式I）然后（iii）将从第二步获得的产物还原在四氢呋喃溶剂中以合成2-二氧基-L-核糖（式III），其中£（Sia）2BH | 用作还原剂。在式（I）中，R和R'分别表示氢或羟基保护基，羟基保护基选自异亚丙基，亚环己基，亚苄基和苄基。

6. 发明授权

KR100930586B1 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르 유도체,이의 제조방법 및 이를 포함하는 약학 조성물 失效
标题翻译： 2-芳基甲基氮杂环丁烷 - 碳青霉烯-3-羧酸酯衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：KR100930586B1
公开(公告)日：2009-12-09
申请号：KR1020070120038
申请日：2007-11-23
申请人： 한국화학연구원 , 국제약품 주식회사
发明人： 김봉진 , 송복주 , 권지웅 , 공재양 , 조희영 , 최영로 , 이동우
IPC分类号： C07D477/20
CPC分类号： Y02A50/473
摘要： 본 발명은 2-아릴메틸아제티딘-카바페넴-3-카복실산의 3번 위치에 특정 구조에 화합물을 에스테르 결합으로 도입한 2-아릴메틸아제티딘-카바페넴-3-카복실산 유도체, 이의 제조방법 및 이를 포함하는 약학 조성물을 제공한다. 상기 2-아릴메틸아제티딘-카바페넴-3-카복실산 유도체는 높은 경구흡수율을 나타냄으로써 경구투여가 가능하며, 그의 활성 대사체는 그람 양성균 및 그람 음성균에 대하여 광범위한 항균 활성을 나타내며, MRSA (메티실린 내성균주) 및 QRS (퀴놀론 내성균주)에 대한 우수한 항균 활성을 나타낸다.
카바페넴
摘要翻译：本发明是为了介绍在以下羧酸的3位上的特定结构的酯键的2-芳基甲基 - 氮杂环丁烷咔唑青霉烯-3-羧酸衍生物，方法它们的制备2-芳基甲基 - 氮杂环丁烷咔唑青霉烯-3-酮化合物和和包含其的药物组合物。通过表达高的口服吸收的2-芳基甲基 - 氮杂环丁烷咔唑青霉烯-3-羧酸衍生物，以及可以口服给药，其活性代谢物显示了针对革兰氏阳性和革兰氏阴性细菌具有广泛的抗菌活性，MRSA（耐甲氧西林耐药菌株）和QRS（喹诺酮耐药菌株）。

7. 发明公开

KR1020090103227A 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르유도체의 산부가염, 이의 제조방법 및 이를 포함하는 약학조성물 失效
标题翻译： 2-亚甲基甜菜碱 - 碳酰基-3-羧酸酯衍生物的添加剂，其制备方法和包含其的药物组合物
公开(公告)号：KR1020090103227A
公开(公告)日：2009-10-01
申请号：KR1020080028691
申请日：2008-03-28
申请人： 국제약품 주식회사 , 한국화학연구원
发明人： 김봉진 , 송복주 , 최영로 , 이범수 , 서동근 , 정영철 , 김시민
IPC分类号： C07D487/04 , C07D403/12
CPC分类号： Y02A50/473
摘要： PURPOSE: An acid addition salt of 2-arylmethylaztidine-carbapenem-3-carboxylate ester derivative is provided to maintain the acid addition salt for a long time with stability. CONSTITUTION: An acid addition salt of 2-arylmethylazetidine-carbapenem-3-carboxylate ester derivative is denoted by the chemical formula 1. In the chemical formula 1, R2 is hydrogen or alkyl group of C1-C4, R2 is straight or branched alkyl group of C1-C12 which is substituted or non-substituted with a cycloalkyl of C4-C7 or cycloalkyl group of C4-C7 which is substituted with alkyl of C1-C4, and n is 0 or 1.
摘要翻译：目的：提供2-芳基甲基氮杂 - 碳青霉烯-3-羧酸酯衍生物的酸加成盐，以保持酸加成盐长期稳定。构成：2-芳基甲基氮杂环丁烷 - 碳青霉烯-3-羧酸酯衍生物的酸加成盐由化学式1表示。在化学式1中，R 2为氢或C 1 -C 4烷基，R 2为直链或支链烷基被C 1 -C 7的环烷基或被C 1 -C 4的烷基取代的C 4 -C 7环烷基取代或未取代的C 1 -C 12，n为0或1。

8. 发明公开

KR1020020042085A (Ｓ)-1-아세틸-2-피롤리딘카복스아미드의 제조방법 失效
标题翻译：制备（S）-1-乙酰基-2-吡咯烷羧酸酰胺的方法
公开(公告)号：KR1020020042085A
公开(公告)日：2002-06-05
申请号：KR1020000071824
申请日：2000-11-30
申请人： 국제약품 주식회사
发明人： 최영로 , 강재효 , 이대원 , 이형주
IPC分类号： C07D207/10
摘要： PURPOSE: A process for preparing (S)-1-acetyl-2-pyrolidine carboxamide, which is useful as an intermediate in synthesis of Levosulpiride, is provided, thereby preparing the subject compound simply in higher yield. CONSTITUTION: The process for preparing (S)-1-acetyl-2-pyrolidine carboxamide comprises the steps of: (a) reacting (S)-proline of formula(2) with acetic acid anhydride, or alternatively (b) reacting (S)-proline of formula(2) with acetic acid anhydride; reacting the reaction compound with acylhalide of formula(3) to prepare a compound of formula(4); and reacting the compound of formula(4) with alcoholic ammonia to prepare (S)-1-acetyl-2-pyrolidine carboxamide of formula(1), wherein X is halogen and R is methyl, ethoxy or t-butyl; the addition mole ratio of the compound of formula(2) and acetic acid anhydride is 1:1 to 1:5; and the acylation is carried out in the presence of base selected from triethylamine, pyridine and dimethylamine.
摘要翻译：目的：提供一种制备（S）-1-乙酰基-2-吡咯烷甲酰胺的方法，其可用作合成左旋肉豆蔻酸的中间体，从而以较高的产率制备本发明化合物。制备（S）-1-乙酰基-2-吡咯烷甲酰胺的方法包括以下步骤：（a）使式（2）的（S） - 脯氨酸与乙酸酐反应，或者（b）使（S ） - 式（2）的脯氨酸与乙酸酐反应; 使反应化合物与式（3）的酰卤反应制备式（4）化合物; 并使式（4）的化合物与醇氨反应制备式（1）的（S）-1-乙酰基-2-吡咯烷甲酰胺，其中X是卤素，R是甲基，乙氧基或叔丁基; 式（2）化合物和乙酸酐的加成摩尔比为1:1至1:5; 并且酰化在选自三乙胺，吡啶和二甲胺的碱的存在下进行。

9. 发明公开

KR1020090053277A 2-아릴메틸아제티딘-카바페넴-3-카복실산 에스테르 유도체,이의 제조방법 및 이를 포함하는 약학 조성물 失效
标题翻译： 2-亚乙基甜菜碱 - 碳酰胺-3-羧酸酯衍生物，其制备方法和包含其的药物组合物
公开(公告)号：KR1020090053277A
公开(公告)日：2009-05-27
申请号：KR1020070120038
申请日：2007-11-23
申请人： 한국화학연구원 , 국제약품 주식회사
发明人： 김봉진 , 송복주 , 권지웅 , 공재양 , 조희영 , 최영로 , 이동우
IPC分类号： C07D477/20
CPC分类号： Y02A50/473
摘要： 본 발명은 2-아릴메틸아제티딘-카바페넴-3-카복실산의 3번 위치에 특정 구조에 화합물을 에스테르 결합으로 도입한 2-아릴메틸아제티딘-카바페넴-3-카복실산 유도체, 이의 제조방법 및 이를 포함하는 약학 조성물을 제공한다. 상기 2-아릴메틸아제티딘-카바페넴-3-카복실산 유도체는 높은 경구흡수율을 나타냄으로써 경구투여가 가능하며, 그의 활성 대사체는 그람 양성균 및 그람 음성균에 대하여 광범위한 항균 활성을 나타내며, MRSA (메티실린 내성균주) 및 QRS (퀴놀론 내성균주)에 대한 우수한 항균 활성을 나타낸다.
카바페넴

10. 发明授权

KR100363566B1 무정형 세푸록심 악세틸의 제조방법 失效
标题翻译： 무정형세푸록심악세틸의제조방법
公开(公告)号：KR100363566B1
公开(公告)日：2003-08-19
申请号：KR1019980049925
申请日：1998-11-20
申请人： 국제약품 주식회사
发明人： 이범수 , 이형주 , 이대원 , 이주희 , 정미란 , 최영로 , 김태훈
IPC分类号： C07D501/26
摘要： PURPOSE: A process for preparing cefuroxime axetil in amorphous form is provided which produces highly pure amorphous cefuroxime axetil in high yields by using water added organic/inorganic salt as a non solvent and reduces the cost of manufacturing because the process to boil up to high temperature is not involved. CONSTITUTION: 5-20 % of crystalline cefuroxime axetil is solubilized with water-miscible organic solvent and adding small quantities of the water containing 0.2-40 % of organic/inorganic salt thereto follows to precipitate at the temperature of 20-30°C. The organic/inorganic salt inhibits the production of crystalline cefuroxime axetil by increasing the polarity of non solvent.
摘要翻译：目的：提供一种以无定形形式制备头孢呋辛酯的方法，该方法通过使用加水有机/无机盐作为非溶剂，以高收率生产高纯度无定形头孢呋辛酯，并且降低了制造成本，因为煮沸至高温不参与。组成：将5-20％的结晶头孢呋辛酯用水混溶性有机溶剂溶解，然后向其中加入少量含有0.2-40％有机/无机盐的水，在20-30℃的温度下沉淀。有机/无机盐通过增加非溶剂的极性来抑制结晶头孢呋辛酯的产生。

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