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1. 发明公开

KR1020080042461A 이미페넴의 제조방법 失效
标题翻译：制备IMIPENEM的方法
公开(公告)号：KR1020080042461A
公开(公告)日：2008-05-15
申请号：KR1020060110940
申请日：2006-11-10
申请人： 제일파마홀딩스 주식회사
发明人： 김문식 , 한창우 , 김종원
IPC分类号： C07D477/20 , C07D487/04
CPC分类号： Y02P20/55 , C07D477/18 , C07D477/20
摘要： A process for the preparation of imipenem is provided to improve preparation yield and purity of imipenem by performing reaction under mild reaction conditions by using an intermediate thienamycin solvate, so that the imipenem is produced in an industrial scale. A process for the preparation of crystalline imipenem monohydrate represented by the formula(I) comprises the steps of: reacting thienamycin solvate represented by the formula(IV) with benzylformimidate represented by the formula(V) in the presence of secondary amine at -40 to -75 deg. C to prepare carboxyl-protected imipenem represented by the formula(VI); hydrogenating the carboxyl-protected imipenem represented by the formula(VI) with 5-10% palladium catalyst in the presence of morpholine or N-methylmorpholine buffer solution at 0-25 deg. C and 4-6 atmospheric pressure; and isolating and crystallizing the reaction product in the presence of ketone solvent, wherein R1 is easily removable carboxyl-protecting group and is selected from benzyl, p-nitrobenzyl and methoxybenzyl; and R2 is alkyl group or aryl group, wherein the thienamycin solvate represented by the formula(IV) is selected from 1,3-dimethyl-2-imidazolidinone(DMI), 1,3-diethyl-2-imidazolidinone(DEI), 1,3-dipropyl-2-imidazolidonone(DPI), 1,3-dibutyl-2-imidazolidinone(DBI), 1,3-diisopropyl-2-imidazolidinone(DIPI) and 1,3-di-t-butyl-2-imidazolidinone(DTBI). Further, the secondary amine is an N,N-diisopropylethylamine.
摘要翻译：提供制备亚胺培南的方法，通过使用中间体噻吩霉素溶剂合物在温和的反应条件下进行反应，从而提高亚胺培南的制备产率和纯度，从而以工业规模生产亚胺培南。由式（I）表示的制备结晶亚胺培南一水合物的方法包括以下步骤：在-40℃存在仲胺的情况下，使式（Ⅳ）代表的噻吩并异恶酮溶剂化物与式（Ⅴ）代表的苄基亚甲酰亚胺反应， -75度制备由式（VI）表示的羧基保护的亚胺培南; 在0-25℃下，在吗啉或N-甲基吗啉缓冲溶液存在下，用5-10％钯催化剂氢化由式（Ⅵ）表示的羧基保护的亚胺培南。 C和4-6大气压; 并在酮溶剂存在下分离和结晶反应产物，其中R 1是容易除去的羧基保护基，并且选自苄基，对硝基苄基和甲氧基苄基; R2为烷基或芳基，其中由式（Ⅳ）表示的噻吩那霉素溶剂合物选自1,3-二甲基-2-咪唑啉酮（DMI），1,3-二乙基-2-咪唑烷酮（DEI），1 ，3-二丙基-2-咪唑啉酮（DPI），1,3-二丁基-2-咪唑啉酮（DBI），1,3-二异丙基-2-咪唑啉酮（DIPI）和1,3-二叔丁基-2-咪唑啉酮咪唑啉酮（DTBI）。此外，仲胺是N，N-二异丙基乙胺。

2. 发明公开

KR1020080093784A 페넴 중간체의 제조방법 失效
标题翻译：笔式中间件的制备方法
公开(公告)号：KR1020080093784A
公开(公告)日：2008-10-22
申请号：KR1020070037991
申请日：2007-04-18
申请人： 성균관대학교산학협력단
发明人： 송충의 , 한상섭
IPC分类号： C07D477/18
CPC分类号： Y02P20/55 , C07D477/18 , B01J23/464 , B01J23/72
摘要： A method for preparing a penem intermediate is provided to decrease the amount of a rhodium catalyst used significantly by using a copper catalyst as an auxiliary catalyst and produce a target product very economically by increasing the efficiency of the rhodium catalyst. A method for preparing a bicyclic keto ester compound represented by a formula(1) from a diazo compound represented by a formula(2) is characterized in that a rhodium catalyst and a copper catalyst, which is copper powder, Cu(I) compound or Cu(II) compound, are simultaneously used. In the formulae(1) and (2), R is a protecting group of a carboxylic acid which is C1-4 alkenyl, or benzyl substituted with para nitro, para C1-4 alkoxy or para C1-6 alkyl; R^1 is H, optionally substituted alkyl, optionally substituted aryl, or optionally substituted heterocyclyl; R^2 is H, acyl or silyl which is tri-substituted with alkyl and aryl, provided that the compound of the formula(1) and the compound of the formula(2) are existent in various optical isomers due to the presence of non-symmetric carbon atoms. In the formula(3), X is O or alkyl-substituted N; and each R1, R2 and R3 is H, C1-30 alkyl or fluorine substituted alkyl.
摘要翻译：提供了一种制备青霉烯中间体的方法，通过使用铜催化剂作为辅助催化剂显着地减少铑催化剂的用量，并通过提高铑催化剂的效率非常经济地制备目标产物。由式（2）表示的重氮化合物制备由式（1）表示的双环酮酯化合物的方法的特征在于，作为铜粉末的铑催化剂和铜催化剂，Cu（I）化合物或 Cu（II）化合物。在式（1）和（2）中，R为羧基的保护基，为C1-4链烯基，或被对硝基，对C1-4烷氧基或对C1-6烷基取代的苄基; R 1是H，任选取代的烷基，任选取代的芳基或任选取代的杂环基; R 2是H，被烷基和芳基三取代的酰基或甲硅烷基，条件是式（1）化合物和式（2）化合物存在于各种光学异构体中，这是由于存在非 - 对称碳原子。在式（3）中，X是O或烷基取代的N; 并且每个R 1，R 2和R 3是H，C 1-30烷基或氟取代的烷基。

3. 发明公开

KR1020050108567A 베타-메틸카바페넴 유도체 및 그의 제조방법 失效
标题翻译： β-甲基胆碱衍生物及其制备方法
公开(公告)号：KR1020050108567A
公开(公告)日：2005-11-17
申请号：KR1020040033474
申请日：2004-05-12
申请人： 한국화학연구원
发明人： 김봉진 , 김재학 , 김광호 , 정희정 , 전미애 , 공재양 , 조희영
IPC分类号： C07D477/20
CPC分类号： Y02P20/55 , C07D477/18 , C07D477/20
摘要： 본 발명은 그람양성균 및 그람음성균에 대해 광범위하게 항균효과를 나타내며, 메티실린 내성 스타필로코쿠스 아우레우스(methicillin resistant staphylococcus aureus, MRSA)를 비롯한 내성균에도 우수한 항균효과를 갖는 하기 화학식 1의 카바페넴 유도체, 이의 제조 방법 및 이를 함유하는 항생제 조성물에 관한 것이다.

상기 식에서, R
1 , R
2 및 R
3 는 각각 독립적으로, 수소, 탄소수 1-3개의 알킬기를 의미하며, M은 수소 또는 약리학적으로 허용가능한 염을 형성하는 짝이온을 나타낸다.

4. 发明授权

KR101031143B1 경구 투여용 카르바페넴 화합물의 신규 합성 중간체 및그의 제조 방법 有权
标题翻译：用于口服给药的卡巴培南化合物的新中间体及其制备方法
公开(公告)号：KR101031143B1
公开(公告)日：2011-04-27
申请号：KR1020057008453
申请日：2003-11-13
申请人： 가부시키가이샤 가네카
发明人： 니시노,게이타 , 고가,데루요시
IPC分类号： C07F9/6561
CPC分类号： C07F9/65611 , C07D205/08 , C07D477/18 , Y02P20/55
摘要： 본 발명은 경구 투여용 1β-메틸카르바페넴 화합물을 효율적으로 제조하기 위한 신규 합성 중간체 및 그의 제조 방법을 제공한다. 즉, 본 발명은 하기 화학식 (5)로 표시되는 β-락탐 화합물을 출발 원료로 하여 하기 화학식 (6)으로 표시되는 화합물과 염기의 존재 하에서 반응시켜 하기 화학식 (1)로 표시되는 신규한 β-락탐 화합물을 얻고, 수산기를 보호한 후, 강염기의 존재 하에서 고리화시키고, 이어서 염화디페닐인산과 반응시킴으로써 하기 화학식 (3)으로 표시되는 신규한 β-락탐 화합물을 얻고, 이것을 탈보호하는 것을 특징으로 하는, 하기 화학식 (4)로 표시되는 신규한 β-락탐 화합물의 제조 방법이다.

(식 중, R
1 은 트리메틸실릴기 또는 트리에틸실릴기이고, R
2 는 아릴기 또는 헤테로아릴기이고, R
3 은 탄소수 1 내지 10의 알킬기 또는 탄소수 3 내지 10의 시클로알킬기이며, X는 할로겐 원자를 나타낸다.)
카르바페넴 화합물, 베타-락탐 화합물, 경구 투여, 중간체

5. 发明公开

KR1020080042460A 티에나마이신 용매화합물 및 그의 제조방법 失效
标题翻译： THIENAMYCIN溶剂及其工艺
公开(公告)号：KR1020080042460A
公开(公告)日：2008-05-15
申请号：KR1020060110939
申请日：2006-11-10
申请人： 제일파마홀딩스 주식회사
发明人： 김문식 , 한창우 , 김종원
IPC分类号： C07D477/20
CPC分类号： Y02P20/55 , C07D477/18 , C07D477/20
摘要： A process for preparing thienamycin solvate useful as an intermediate for preparing imipenem is provided to improve preparation yield and convenience and purity of the compound by using easily obtainable raw materials and reagents and performing the reaction under mild condition. A process for preparing thienamycin solvate represented by the formula(IV) comprises the steps of: reacting compounds represented by the formula(II) with diphenylchloro phosphate in a solvent selected from 1,3-dimethyl-2-imidazolidinone(DMI), 1,3-diethyl-2-imidazolidinone(DEI), 1,3-dipropyl-2-imidazolidonone(DPI), 1,3-dibutyl-2-imidazolidinone(DBI), 1,3-diisopropyl-2-imidazolidinone(DIPI) and 1,3-di-t-butyl-2-imidazolidinone(DTBI) or a mixture of the solvent with dichloromethane in the presence of secondary amine at -10 to -60 deg. C; and coupling the reaction product with 2-aminoethanthiol or its hydrochlorate under in-situ reaction condition, wherein R1 is easily removable carboxyl-protecting group and is selected from benzyl, p-nitrobenzyl and methoxybenzyl; and R2 is alkyl group or aryl group. Further, the secondary amine is an N,N-diisopropylethylamine.
摘要翻译：提供一种制备用作制备亚胺培南的中间体的噻吩那霉素溶剂化物的方法，通过使用容易获得的原料和试剂，并在温和条件下进行反应，提高了化合物的制备产率和方便性和纯度。制备由式（Ⅳ）表示的噻吩那霉素溶剂合物的方法包括以下步骤：使式（II）表示的化合物与选自1,3-二甲基-2-咪唑啉酮（DMI），（DEI），1,3-二丙基-2-咪唑啉酮（DPI），1,3-二丁基-2-咪唑啉酮（DBI），1,3-二异丙基-2-咪唑啉酮（DIPI）和 1,3-二叔丁基-2-咪唑烷酮（DTBI）或溶剂与二氯甲烷的混合物在仲胺的存在下在-10至-60℃下进行。 C; 并在原位反应条件下将反应产物与2-氨基硫醇或其盐酸盐偶合，其中R1是容易除去的羧基保护基团，选自苄基，对硝基苄基和甲氧基苄基; 并且R 2是烷基或芳基。此外，仲胺是N，N-二异丙基乙胺。

6. 发明公开

KR1020090007572A 카르바페넴 항생 물질 중간체의 개량된 정석 방법 无效
标题翻译：碳水化合物抗生素中间体结晶的改进方法
公开(公告)号：KR1020090007572A
公开(公告)日：2009-01-19
申请号：KR1020087026255
申请日：2007-04-18
申请人： 카네카 코포레이션
发明人： 니시노게이타 , 고가데루요시 , 후카에마사후미 , 우에다야스요시
IPC分类号： C07F9/09 , C07D477/00
CPC分类号： C07F9/65611 , C07D477/18
摘要： The invention provides a method for crystallization by which azetidinone compounds extremely useful as the common intermediate for the synthesis of 1beta-methylcarbapenem compounds can be obtained as stable crystals which have higher quality than that of conventional ones and are excellent in the filterability in recovery of crystals; azetidinone compounds lowered in the content of impurities; and azetidinone compounds which are controlled in the particle size distribution of crystals and improved in handleability and stability. The method comprises adding a hydrocarbon solvent to a solution of an azetidinone compound extremely useful as the common intermediate for the synthesis of 1beta-methylcarbapenem compounds in the presence of at most 200wt% of seed crystals based on the weight of the azetidinone compound. According to the method, high-quality and stable crystals excellent in the filterability in recovery of crystals can be obtained.
摘要翻译：本发明提供一种结晶方法，通过该方法可以获得作为合成1,1-甲基碳青霉烯化合物的常用中间体的非常有用的氮杂环丁酮化合物，其具有比常规晶体更高质量的稳定晶体，并且在晶体回收过程中具有优异的过滤性 ; 氮杂环丁酮化合物杂质含量降低; 和氮杂环丁酮化合物，其被控制在晶体的粒度分布中并且改善了可操作性和稳定性。该方法包括在基于氮杂环丁酮化合物的重量存在下存在至多200wt％晶种的情况下，将一种烃溶剂加入到作为用于合成1'-甲基碳青霉烯化合物的常用中间体的氮杂环丁酮化合物溶液中。根据该方法，可以获得晶体回收过滤性优异且稳定的晶体。

7. 发明公开

KR1020050075392A 경구 투여용 카르바페넴 화합물의 신규 합성 중간체 및그의 제조 방법 有权
标题翻译：用于口服给药的碳水化合物的新型中间体及其生产方法
公开(公告)号：KR1020050075392A
公开(公告)日：2005-07-20
申请号：KR1020057008453
申请日：2003-11-13
申请人： 가부시키가이샤 가네카
发明人： 니시노,게이타 , 고가,데루요시
IPC分类号： C07F9/6561
CPC分类号： C07F9/65611 , C07D205/08 , C07D477/18 , Y02P20/55
摘要： A novel intermediate which is for use in efficiently producing a 1beta-methylcarbapenem compound for oral administration; and a process for producing the intermediate. The process, which is for producing a novel beta-lactam compound represented by the general formula (4), is characterized by reacting a beta-lactam compound represented by the general formula (5) as a starting material with a compound represented by the general formula (6) in the presence of a base to obtain a novel beta-lactam compound represented by the general formula (1), protecting the hydroxy group, subsequently cyclizing the protected compound in the presence of a strong base, reacting the cyclized compound with diphenylphosphoryl chloride to obtain a novel beta-lactam compound represented by the general formula (3), and removing the protective group therefrom. (5) (6) (1) (3) (4) (In the formulae, R1 represents trimethylsilyl or triethylsilyl; R2 represents aryl or heteroaryl; R3 represents C1-10 alkyl or C3- 10 cycloalkyl; and X represents halogeno.)
摘要翻译：一种用于口服给药的高效制备1β-甲基碳青霉烯化合物的新型中间体; 和中间体的制造方法。用于生产由通式（4）表示的新型β-内酰胺化合物的方法的特征在于使由通式（5）表示的β-内酰胺化合物作为起始原料与通式式（6）的化合物，得到由通式（1）表示的新型β-内酰胺化合物，保护羟基，随后在强碱存在下环化受保护的化合物，使环化的化合物与二苯基磷酰氯，得到通式（3）表示的新型β-内酰胺化合物，除去保护基。（5）（6）（1）（3）（4）（式中，R1表示三甲基甲硅烷基或三乙基甲硅烷基; R 2表示芳基或杂芳基; R 3表示C 1-10烷基或C 3-10环烷基; X表示卤代。

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