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1. 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

2. 发明授权

KR100451670B1 내성균에 대해 항생작용을 갖는 카바페넴 유도체 및 이의제조방법 失效
标题翻译： 내성균에대해항생작용을갖갖는카바페넴유도체및이의제조방
公开(公告)号：KR100451670B1
公开(公告)日：2004-10-08
申请号：KR1020010056740
申请日：2001-09-14
申请人： 한국화학연구원
发明人： 김봉진 , 이철해 , 김재학 , 정희정 , 편도규 , 전미애 , 권지웅 , 김현주
IPC分类号： C07D477/14
CPC分类号： Y02P20/55
摘要： PURPOSE: Provided are carbapenem derivatives represented by formula(1) and a preparation method thereof. The carbapenem derivatives have antibacterial activity against the resistant strains such as methicillin resistant Staphylococcus aureus(MRSA) and resistant strain against Ofloxacin. CONSTITUTION: The method of preparation comprises: reacting a compound of formula(2) with a compound of formula(3) to make an ester derivatives of carbapenem represented by formula(4); and de-protecting carboxy group and hydroxy group. In formula(1), X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group, or C1-2 alkoxy group; M is hydrogen atom or a pair ion forming a pharmaceutically allowable salt. In formula(2,3 and 4), R1 is hydrogen atom or hydroxy protecting group; R2 is carboxy protecting group; X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group.
摘要翻译：用途：提供了由式（1）表示的碳代青霉烯衍生物及其制备方法。碳青霉烯衍生物对耐药菌株如耐甲氧西林金黄色葡萄球菌（MRSA）和抗氧氟沙星耐药菌株具有抗菌活性。构成：制备方法包括：使式（2）化合物与式（3）化合物反应，制得式（4）代表的碳青霉烯酯衍生物; 和去保护羧基和羟基。在式（1）中，X是S或O原子; Y是在苯基中的某个位置上的氢或卤素原子，或C1-2烷氧基; M是氢原子或形成药学上允许的盐的一对离子。在式（2,3和4）中，R 1是氢原子或羟基保护基; R2是羧基保护基; X是S或O原子; Y在苯基的某个位置上是氢或卤素原子。

3. 发明公开

KR1020030023968A 내성균에 대해 항생작용을 갖는 카바페넴 유도체 및 이의제조방법 失效
标题翻译：具有耐药菌株抗菌活性的碳水化合物及其制备方法
公开(公告)号：KR1020030023968A
公开(公告)日：2003-03-26
申请号：KR1020010056740
申请日：2001-09-14
申请人： 한국화학연구원
发明人： 김봉진 , 이철해 , 김재학 , 정희정 , 편도규 , 전미애 , 권지웅 , 김현주
IPC分类号： C07D477/14
CPC分类号： Y02P20/55
摘要： PURPOSE: Provided are carbapenem derivatives represented by formula(1) and a preparation method thereof. The carbapenem derivatives have antibacterial activity against the resistant strains such as methicillin resistant Staphylococcus aureus(MRSA) and resistant strain against Ofloxacin. CONSTITUTION: The method of preparation comprises: reacting a compound of formula(2) with a compound of formula(3) to make an ester derivatives of carbapenem represented by formula(4); and de-protecting carboxy group and hydroxy group. In formula(1), X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group, or C1-2 alkoxy group; M is hydrogen atom or a pair ion forming a pharmaceutically allowable salt. In formula(2,3 and 4), R1 is hydrogen atom or hydroxy protecting group; R2 is carboxy protecting group; X is S or O atom; Y is hydrogen or halogen atom on a certain location in phenyl group.
摘要翻译：目的：提供式（1）表示的碳青霉烯衍生物及其制备方法。碳青霉烯衍生物对抗性菌株如耐甲氧西林金黄色葡萄球菌（MRSA）和耐氧沙星的抗性菌株具有抗菌活性。构成：制备方法包括：使式（2）化合物与式（3）化合物反应，制得由式（4）表示的碳青霉烯的酯衍生物; 并脱保护羧基和羟基。在式（1）中，X是S或O原子; Y是苯基或C1-2烷氧基中某一位置上的氢或卤素原子; M是氢原子或形成药学上允许的盐的成对离子。在式（2,3和4）中，R 1是氢原子或羟基保护基; R2是羧基保护基; X是S或O原子; Y是苯基中某一位置的氢或卤素原子。

4. 发明公开

KR1020080095476A 베타-메틸아제티디논의 제조방법 无效
标题翻译：制备BETA-METHYLAZETIDINONE的方法
公开(公告)号：KR1020080095476A
公开(公告)日：2008-10-29
申请号：KR1020070039998
申请日：2007-04-24
申请人： 한국화학연구원
发明人： 김봉진 , 권지웅 , 허정희
IPC分类号： C07D205/08
摘要： A method of manufacturing the beta-methyl azetidinone is provided to produce easily the beta-methyl azetidinone without using 4-acetoxyazetidinone which is used to synthesize the beta-methyl. The beta-methyl azetidinone is obligatorily used in order to manufacture carbapenem antibiotics. A compound of a chemical formula 5 is manufactured by reacting a compound of a chemical formula 2 with the cubic aiding agent of a chemical formula 3 or 4 and zinc powders in an organic solvent. The compound of the chemical formula 5 is reacted with the hydrogen peroxide and lithiumhydroxide in the organic solvent. In the chemical formulae, R the tert-butyl dimethylsilyl, R2 phenyl or cyclopropyl, and AUX is the cubic aiding agent.
摘要翻译：提供了制备β-甲基氮杂环丁酮的方法以容易地生产β-甲基氮杂环丁酮，而不使用用于合成β-甲基的4-乙酰氧基氮杂环丁酮。为了制造碳青霉烯类抗生素，必须使用β-甲基氮杂环丁酮。通过使化学式2的化合物与化学式3或4的立方辅助试剂和锌粉末在有机溶剂中反应来制备化学式5的化合物。化学式5的化合物与有机溶剂中的过氧化氢和氢氧化锂反应。在化学式中，R为叔丁基二甲基甲硅烷基，R2苯基或环丙基，AUX为立方体助剂。

5. 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）。

6. 发明授权

KR100441901B1 세팔로스포린 유도체의 개선된 제조방법 失效
标题翻译： 세팔로스포린유도체의개선된제조방법
公开(公告)号：KR100441901B1
公开(公告)日：2004-07-27
申请号：KR1020010039222
申请日：2001-07-02
申请人： 한국화학연구원 , 일동홀딩스(주)
发明人： 이철해 , 김봉진 , 강재훈 , 편도규 , 김재학 , 정희정 , 전미애 , 정원장 , 권지웅 , 박용엽 , 김기원
IPC分类号： C07D501/57
摘要： PURPOSE: Provided is an improved process for the preparation of cephalosporin derivatives from (cis)-3-acetoxypropen-cephalosporinic acid in higher yield. CONSTITUTION: The improved process for the preparation of cephalosporin derivative of the formula(1) comprises the steps of: radical reaction of a compound of the formula(5) with benzenthiol and azobisisobutyronitrile as a radical initiator in an organic solvent to convert it into a trans form; continuous reaction of the reaction product with a compound of the formula(10) to obtain a compound of the formula(3); and reaction of the compound of the formula(3) with an acylated compound of the formula(8) and a silylated compound of the formula(9).
摘要翻译：目的：提供一种由（顺式）-3-乙酰氧基丙烯酸头孢菌素酸以较高产率制备头孢菌素衍生物的改进方法。构成：制备式（1）头孢菌素衍生物的改进方法包括以下步骤：将式（5）化合物与苯硫醇和偶氮二异丁腈作为自由基引发剂在有机溶剂中进行自由基反应，将其转化为转变; 使反应产物与式（10）化合物连续反应，得到式（3）化合物; 和式（3）化合物与式（8）酰化化合物和式（9）甲硅烷基化化合物的反应。

7. 发明公开

KR1020030002925A 세팔로스포린 유도체의 개선된 제조방법 失效
标题翻译：改进CEPHOROSPORIN衍生物的制备方法
公开(公告)号：KR1020030002925A
公开(公告)日：2003-01-09
申请号：KR1020010039222
申请日：2001-07-02
申请人： 한국화학연구원 , 일동홀딩스(주)
发明人： 이철해 , 김봉진 , 강재훈 , 편도규 , 김재학 , 정희정 , 전미애 , 정원장 , 권지웅 , 박용엽 , 김기원
IPC分类号： C07D501/57
摘要： PURPOSE: Provided is an improved process for the preparation of cephalosporin derivatives from (cis)-3-acetoxypropen-cephalosporinic acid in higher yield. CONSTITUTION: The improved process for the preparation of cephalosporin derivative of the formula(1) comprises the steps of: radical reaction of a compound of the formula(5) with benzenthiol and azobisisobutyronitrile as a radical initiator in an organic solvent to convert it into a trans form; continuous reaction of the reaction product with a compound of the formula(10) to obtain a compound of the formula(3); and reaction of the compound of the formula(3) with an acylated compound of the formula(8) and a silylated compound of the formula(9).
摘要翻译：目的：提供从（顺式）-3-乙酰氧基丙基 - 头孢菌酸制备头孢菌素衍生物的较高产率的改进方法。构成：制备式（1）的头孢菌素衍生物的改进方法包括以下步骤：将式（5）化合物与苯并二酚和偶氮二异丁腈作为自由基引发剂在有机溶剂中进行自由基反应，将其转化为转变; 反应产物与式（10）化合物的连续反应，得到式（3）化合物; 和式（3）的化合物与式（8）的酰化化合物和式（9）的甲硅烷基化合物的反应。

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