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公开(公告)号：KR1020110070523A
公开(公告)日：2011-06-24
申请号：KR1020090127380
申请日：2009-12-18
Applicant: 한국과학기술연구원
IPC: C12P35/00 , A61K31/545
CPC classification number: C12P35/06 , A61K31/545 , C07B2200/13 , C07D501/16 , C12N9/84 , C12Y305/01011
Abstract: PURPOSE: A method for preparing a cephalosporin antibiotics intermediate using a novel enzyme is provided to industrially synthesize an acrystalline hydrate. CONSTITUTION: A method for preparing cephalosporin antibiotic intermediate of chemical formula 1 comprises: a step of adding cresol or phenol to a compound of chemical formula 2 and stirring to deprotecting a protection group of carboxyl groups; a step of adjusting pH concentration with a base, adding Sinta CLEC-PA enzyme, and deprotecting; and a step of adjusting pH concentration with inorganic acid. The base is a carbonate alkali metal, alkali metal hydroxide, ammonia solution, or trialkyl amine.
Abstract translation: 目的：提供一种使用新型酶制备头孢菌素抗生素中间体的方法，用于工业合成结晶水合物。 构成：化学式1的头孢菌素抗生素中间体的制备方法包括：向化学式2的化合物中加入甲酚或苯酚并搅拌使保护基脱羧的步骤; 用碱调节pH浓度，添加Sinta CLEC-PA酶，脱保护的步骤; 以及用无机酸调节pH浓度的步骤。 碱为碳酸碱金属，碱金属氢氧化物，氨溶液或三烷基胺。
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公开(公告)号：KR100717131B1
公开(公告)日：2007-05-11
申请号：KR1020050103572
申请日：2005-10-31
Applicant: 한국과학기술연구원
IPC: C07D487/04
Abstract: 본 발명은 1-베타메틸카바페넴 유도체 및 그 제조에 사용되는 중간체에 관한 것으로서, 상기 1-베타메틸카바페넴 유도체는 하기 화학식 1의 구조를 갖는 것을 특징으로 한다.
(상기 화학식 (I)에서, X는 O, S, N 이고, Y는 옥소, 히드록시, 옥심, 메톡시이민이다.)
본 발명에 의한 1-베타메틸카바페넴 유도체는 시클릭아민기가 포함된 티올 유도체를 치환시킴으로써 항균 활성이 우수하고, 내성균에 강한 효과가 있다. 따라서 본 발명에 의한 1-베타메틸카바페넴 유도체는 항생제로서 유용하게 사용할 수 있다.
항생제, 카바페넴, 사이클릭아민, 피롤리딘Abstract translation: 本发明的特征在于具有的1-β甲基碳青霉烯衍生物青霉烯的结构具有下式1涉及的1-β甲基碳青霉烯衍生物青霉烯和它的生产中使用的中间体。
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公开(公告)号：KR100510587B1
公开(公告)日：2005-08-30
申请号：KR1020010088951
申请日：2001-12-31
Applicant: 한국과학기술연구원
IPC: C07C41/52
Abstract: 본 발명은 할로겐이 치환된 디페닐에테르 유도체의 제조방법에 관한 것으로, 더욱 구체적으로 디페닐에테르 화합물을 출발물질로 하여 산용액하에서 할로겐산나트륨을 혼합하여 할로겐화하는 단계; 프리델-크래프트 아실화 반응을 수행하는 단계; 과산화 수소와 무수말린산을 이용하여 산화시키는 단계; 및 가수분해 단계로 이루어진 할로겐이 치환된 디페닐에테르 유도체의 제조방법에 관한 것으로, 종래 염소화 반응에서 사용되는 염소기체 대신 할로겐산나트륨 및 산용액을 사용하므로, 대규모 생산하는데 있어서 비용 및 제조시간이 절약되며, 정량적인 반응에 의해 부생성물을 줄일 수 있으며, 이로 인해 수율을 더욱 높일 수 있으며, 또한 전 과정에서 단일 용매를 사용할 수 있어 공정상의 조작을 단순히 하여 경제성 있는 제조방법이다.
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公开(公告)号：KR100441764B1
公开(公告)日：2004-07-27
申请号：KR1020000087303
申请日：2000-12-30
Applicant: 한국과학기술연구원
IPC: C07C247/08
Abstract: PURPOSE: Provided is a vinyl carbamoyl azide derivative, which is more stable than a conventional carbamoyl azide derivative and has an effective sterilizing power against mold harmful to the crops. CONSTITUTION: The vinyl carbamoyl azide derivative represented by the formula 1 is produced by reacting an isocyanate compound(R1NCO) and hydrazoic acid(NH3) or sodium azide(NaN3). In the formula, R1 is at least one C1-C6 alkyl, or furyl or phenyl capable of being substituted by at least one substituent selected from the group consisting of halogen, C1-C6 alkoxy, and nitro.
Abstract translation: 用途：提供一种比常规氨基甲酰叠氮衍生物更稳定的乙烯基氨基甲酰基叠氮化物衍生物，并且具有对作物有害的霉菌有效的杀菌力。 构成：由式1表示的乙烯基氨基甲酰基叠氮化物衍生物通过使异氰酸酯化合物（R1NCO）和叠氮酸（NH3）或叠氮化钠（NaN3）反应来制备。 在该式中，R1是至少一个C1-C6烷基，或者能被至少一个选自卤素，C1-C6烷氧基和硝基的取代基取代的呋喃基或苯基。
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公开(公告)号：KR1020030058496A
公开(公告)日：2003-07-07
申请号：KR1020010088951
申请日：2001-12-31
Applicant: 한국과학기술연구원
IPC: C07C41/52
Abstract: PURPOSE: A method for preparing a diphenyl ether derivative substituted with halogen is provided, to reduce the cost and the preparation time by employing a sodium salt of halogen acid and an acid solution instead of chlorine gas, to reduce the amount of by-product and to improve the yield. CONSTITUTION: The method comprises the steps of reacting diphenyl ether represented by the formula 2 with sodium salt of halogen acid in the presence of an acid solution to prepare 2,4,4'-trihalogen diphenyl ether represented by the formula 3; reacting the obtained compound of the formula 3 with acetyl chloride in the presence of an aluminium catalyst to prepare 2,4,4'-trihalogen-2'-acetyldiphenyl ether represented by the formula 4; reacting the obtained compound of the formula 4 with maleic anhydride in the presence of hydrogen peroxide to prepare 2,4,4'-trihalogen-2'-acetoxydiphenyl ether represented by the formula 5; and reacting the obtained compound of the formula 5 with a strong base to prepare 2,4,4'-trihalogen-2'-hydroxydiphenyl ether represented by the formula 1, wherein X is Cl or Br.
Abstract translation: 目的：提供一种制备被卤素取代的二苯基醚衍生物的方法，通过使用卤酸钠和酸溶液代替氯气来降低成本和制备时间，以减少副产物的量和 提高产量。 方案：该方法包括在酸溶液存在下使由式2表示的二苯醚与卤酸钠盐反应制备由式3表示的2,4,4'-三卤代二苯醚; 在铝催化剂存在下，使所得到的式3化合物与乙酰氯反应，制得式4表示的2,4,4'-三卤代-2'-乙酰基二苯基醚; 所得到的式4化合物与过氧化氢存在下的马来酸酐反应制备式5表示的2,4,4'-三卤素-2'-乙酰氧基二苯醚; 并使所得式5的化合物与强碱反应，制备由式1表示的2,4,4'-三卤代-2'-羟基二苯醚，其中X为Cl或Br。
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Patent Agency Ranking
公开(公告)号：KR100388432B1
公开(公告)日：2003-06-25
申请号：KR1020000087302
申请日：2000-12-30
Applicant: 한국과학기술연구원
IPC: C07F9/38
Abstract: PURPOSE: Provided is a manufacturing method for dialkyl(4-hydroxy-3,5-di(t-butyl)benzyl)phosphonate(DAP) in high yield , thereby mass-producing DAP without generating carcinogens not by using a strong base. CONSTITUTION: Dialkyl(4-hydroxy-3,5-di(t-butyl)benzyl)phosphonate is manufactured by reacting N, N-dialkyl-(4-hydroxy-3,5-di(t-butyl)benzyl)amine or its salt with dialkyl phosphate or trialkyl phosphate in the presence of an alkylating agent, at 60-120 deg.C.
Abstract translation: 目的：提供高收率地制备（4-羟基-3,5-二（叔丁基）苄基）膦酸二烷基酯（DAP）的方法，由此不用强碱就可以大量生产DAP而不产生致癌物质。 构成：通过N，N-二烷基 - （4-羟基-3,5-二（叔丁基）苄基）胺或 其在烷基化试剂存在下与磷酸二烷基酯或磷酸三烷基酯在60-120℃下进行反应。
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公开(公告)号：KR1020030015551A
公开(公告)日：2003-02-25
申请号：KR1020010049334
申请日：2001-08-16
Applicant: 한국과학기술연구원
IPC: C07D487/06
Abstract: PURPOSE: Provided are antibiotic 1-β-methyl-carbapenem derivatives of the formula(2) substituted with novel bicyclic thiol derivatives represented by the formula(1) which have stability against DHP-1 enzyme and are effective against resistant bacteria. CONSTITUTION: The method for preparing thiols and carbapenem derivatives comprises the steps of: carrying on the reaction scheme(1) to make thiols and combining them with carbapenem derivatives to make the final product of the formula(2). In the formula(1) and the formula(2), R1 is methyl or ethyl group and R2 is C1-6 alkyl such as methyl, ethyl, propyl, C1-6 cycloalkyl or alkyl substituted with phenyl, vinyl and hydroxyl group.
Abstract translation: 目的：提供式（2）的抗生素1-β-甲基 - 碳青霉烯衍生物，其由式（1）表示的新型双环硫醇衍生物取代，其具有对DHP-1酶的稳定性并且对抗细菌有效。 构成：制备硫醇和碳青霉烯衍生物的方法包括以下步骤：进行反应方案（1）制备硫醇并与碳青霉烯衍生物结合，制得式（2）的最终产物。 在式（1）和式（2）中，R 1是甲基或乙基，R 2是C 1-6烷基，例如甲基，乙基，丙基，C 1-6环烷基或被苯基，乙烯基和羟基取代的烷基。
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公开(公告)号：KR1020010081711A
公开(公告)日：2001-08-29
申请号：KR1020000007775
申请日：2000-02-18
Applicant: 한국과학기술연구원
IPC: C02F3/34
Abstract: PURPOSE: A COD(chemical oxygen demand) reducing technology for leachate from a reclamation site using biological treatment is provided to greatly reduce COD by using bacteria producing lignin decomposition and/or oxidation enzyme. CONSTITUTION: Using bacteria having lignin decomposing enzyme or oxidizing enzyme like monoxidase or dioxidase, lignin and cyclic compounds containing halogen, which are hardly decomposed under normal condition, are easily decomposed to reduce COD. The treated bacteria grow well without adding no nutrient in the leachate. Intake and decomposition by the bacteria reduce COD value and lower nutrients in the leachate.
Abstract translation: 目的：提供使用生物处理从填埋场渗滤液的COD（化学需氧量）减少技术，通过使用细菌生产木质素分解和/或氧化酶大大降低COD。 构成：使用具有木质素分解酶或氧化酶如单氧化物酶或氧化酶的细菌，在正常条件下难以分解的含有卤素的木质素和环状化合物容易分解以降低COD。 经处理的细菌生长良好，不会在渗滤液中添加营养物质。 细菌的摄入和分解降低了COD值，降低了浸出液中的营养。
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