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公开(公告)号：KR100441901B1
公开(公告)日：2004-07-27
申请号：KR1020010039222
申请日：2001-07-02
IPC: C07D501/57
Abstract: 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).
Abstract translation: 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。
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公开(公告)号：KR1020030002925A
公开(公告)日：2003-01-09
申请号：KR1020010039222
申请日：2001-07-02
IPC: C07D501/57
Abstract: 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).
Abstract translation: 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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公开(公告)号：KR1020020079654A
公开(公告)日：2002-10-19
申请号：KR1020020052421
申请日：2002-09-02
IPC: C07D265/22
Abstract: PURPOSE: Provided are azetidinone compound of the formula(I) as an intermediate useful for the manufacture of carbapenem antibiotics and a process for the preparation thereof. CONSTITUTION: The azetidine compound is represented by the formula(I). It is useful as an intermediate for the manufacture of beta-methylcarbapenem antibiotics and manufactured by reacting 4-acetoxy-azetidine compound of the formula(II) and alpha-halo propionic acid amide compound of the formula(III).
Abstract translation: 目的：提供式（I）的氮杂环丁酮化合物作为制备碳青霉烯类抗生素的中间体及其制备方法。 构成：氮杂环丁烷化合物由式（I）表示。 通过使式（II）的4-乙酰氧基 - 氮杂环丁烷化合物与式（III）的α-卤代丙酸酰胺化合物反应制备β-甲基碳青霉烯类抗生素的中间体是有用的。
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公开(公告)号：KR1020030023968A
公开(公告)日：2003-03-26
申请号：KR1020010056740
申请日：2001-09-14
Applicant: 한국화학연구원
IPC: C07D477/14
CPC classification number: Y02P20/55
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：KR1020020006889A
公开(公告)日：2002-01-26
申请号：KR1020000040396
申请日：2000-07-14
Applicant: 한국화학연구원
IPC: C07D205/08
Abstract: PURPOSE: Provided are 2-arylethenyl carbapenem derivative of the formula(1) and its pharmaceutically acceptable salt which have therapeutic effect in methicillin resistant staphylococcus aureus(MRSA) infection. And its manufacturing method and an antibacterial composition containing it as an active ingredient are also provided. CONSTITUTION: 2-arylethenyl carbapenem derivative is represented by the formula(1), wherein R is halogen, nitro, hydroxy or cyano substituted phenyl or fused aryl group; or halogen or C1-3 alkyl group substituted monocyclic, bicyclic or tricyclic 5 or 6 membered hetero aryl group containing at least one of O, S or N atom; and M is hydrogen or zwitterion forming pharmaceutically acceptable salts.
Abstract translation: 目的：提供式（1）的2-亚乙烯基碳青霉烯衍生物及其药用盐，其在耐甲氧西林金黄色葡萄球菌（MRSA）感染中具有治疗作用。 还提供其制造方法和含有它作为活性成分的抗菌组合物。 构成：2-亚乙烯基碳代青霉烯衍生物由式（1）表示，其中R是卤素，硝基，羟基或氰基取代的苯基或稠合芳基; 或含有O，S或N原子中的至少一个的卤素或C 1-3烷基取代的单环，双环或三环5或6元杂芳基; M是氢或两性离子形成药学上可接受的盐。
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Patent Agency Ranking
公开(公告)号：KR100231498B1
公开(公告)日：1999-11-15
申请号：KR1019970060989
申请日：1997-11-19
Applicant: 한국화학연구원
IPC: C07D471/04
Abstract: 본 발명은 그람 양성균은 물론 녹농균을 제외한 그람 음성균에 대하여 우수한 항균 작용을 나타내는, 하기 화학식 1a 또는 화학식 1b로 표시되는 카르바페넴 유도체 화합물, 이의 제조 방법 및 이를 포함하는 약제학적 조성물을 제공한다.
식 중, R은 수소, 카르복실 음이온, 카르복실 보호기, 또는 제약학상 허용가능한 무기 또는 유기염이고, R
1 은 수소 또는 히드록시 보호기이며, R
2 는 C
1 내지 C
5 의 시클릭 또는 비시클릭 저급 알킬기 또는 방향족 알킬기이거나, 또는 질소, 황 및 산소로 이루어지는 군으로부터 선택된 1개 이상의 헤테로 원자를 함유하는 모노 또는 비시클릭, 포화 또는 불포화 고리인, 임의 치환된 헤테로시클릭 라디칼이고, R
3 은 수소, C
1 내지 C
5 의 시클릭 또는 비시클릭 저급 알킬기, 카르바모일기 또는 아세틸기이다.-
公开(公告)号：KR100446432B1
公开(公告)日：2004-08-30
申请号：KR1020010048742
申请日：2001-08-13
Applicant: 한국화학연구원
IPC: C07D417/14
CPC classification number: Y02P20/55
Abstract: PURPOSE: Provided are 2-benzothiazole carbapenem derivatives represented by the formula 1, a preparation method thereof and the composition containing the same. The composition has an excellent antibiotic property and is effective against resistant bacteria such as methicillin resistant Staphylococcus Aureus, MRSA and ofloxacin resistant Staphylococcus Aureus(QRSA). CONSTITUTION: In the carbapenem derivatives represented by the formula 1, M is hydrogen or a pair ion forming pharmaceutically allowed salts. The synthetic rout comprises reacting a compound of the formula 2 with a compound of the formula 3 to make a compound of the formula 4, and eliminating the carboxy protecting group from it. In the formula 4, R1 is a hydroxy protecting group such as tert-butyl silyl or triethylsilyl group; R2 is a carboxy protecting group such as p-nitrobenzyl, aryl or p-methoxybenzyl; R3 is an amine protecting group such as aryloxy carbonyl or p-nitrobenzyloxy carbonyl.
Abstract translation: 目的：提供由式1表示的2-苯并噻唑碳青霉烯衍生物，其制备方法和含有其的组合物。 该组合物具有优异的抗生素性质，并且对抵抗性细菌例如耐甲氧西林金黄色葡萄球菌，MRSA和耐氧氟沙星金黄色葡萄球菌（QRSA）是有效的。 构成：在由式1表示的碳代青霉烯衍生物中，M为氢或形成药学允许盐的一对离子。 合成路线包括将式2的化合物与式3的化合物反应以制备式4的化合物，并从其中除去羧基保护基。 式4中，R 1为羟基保护基，例如叔丁基甲硅烷基或三乙基甲硅烷基; R2是羧基保护基，如对硝基苄基，芳基或对甲氧基苄基; R3是胺保护基团，如芳氧基羰基或对硝基苄氧基羰基。
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公开(公告)号：KR100385364B1
公开(公告)日：2003-05-27
申请号：KR1020020052421
申请日：2002-09-02
IPC: C07D265/22
Abstract: PURPOSE: Provided are azetidinone compound of the formula(I) as an intermediate useful for the manufacture of carbapenem antibiotics and a process for the preparation thereof. CONSTITUTION: The azetidine compound is represented by the formula(I). It is useful as an intermediate for the manufacture of beta-methylcarbapenem antibiotics and manufactured by reacting 4-acetoxy-azetidine compound of the formula(II) and alpha-halo propionic acid amide compound of the formula(III).
Abstract translation: 目的：提供式（I）的氮杂环丁酮化合物作为可用于制备碳青霉烯类抗生素的中间体及其制备方法。 构成：氮杂环丁烷化合物由式（I）表示。 它可用作制备β-甲基碳青霉烯类抗生素的中间体，并通过使式（II）的4-乙酰氧基 - 氮杂环丁烷化合物与式（III）的α-卤代丙酰胺化合物反应制备。
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公开(公告)号：KR100451670B1
公开(公告)日：2004-10-08
申请号：KR1020010056740
申请日：2001-09-14
Applicant: 한국화학연구원
IPC: C07D477/14
CPC classification number: Y02P20/55
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：KR1020020013988A
公开(公告)日：2002-02-25
申请号：KR1020000046447
申请日：2000-08-10
IPC: C07D413/14
CPC classification number: C07D413/06 , C07D205/08 , C07D265/06 , C07D265/14 , C07D487/04 , C07F9/65611 , Y02P20/55
Abstract: PURPOSE: Provided is an intermediate, azetidinone compound which is useful in manufacturing beta-methylcarbapenem antibiotics. And its manufacturing method is provided. CONSTITUTION: The intermediate of carbapenem, azetidinone compound, is represented by the formula(1), wherein R is hydrogen or hydroxy protective group, R1 and R2 are individually C1-C15 alkyl, benzyl, represent 5-6 membered cyclic compound to which R1 and R2 are linked, or hetero cyclic group including at least one oxygen or sulfur atom; R3 is lower alkyl group or lower alkylester group; and R4 is benzene, halogen, lower alkyloxy group, or nitro group substituted benzene ring.
Abstract translation: 目的：提供可用于制备β-甲基碳青霉烯类抗生素的中间体氮杂环丁酮化合物。 并提供其制造方法。 构成：碳青霉烯类氮杂环丁酮化合物的中间体由式（1）表示，其中R是氢或羟基保护基，R1和R2分别是C1-C15烷基，苄基，代表5-6元环状化合物，其中R1 或R 2连接，或包含至少一个氧原子或硫原子的杂环基; R3是低级烷基或低级烷基酯基; R4为苯，卤素，低级烷氧基或硝基取代苯环。
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