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公开(公告)号：KR1020010077073A
公开(公告)日：2001-08-17
申请号：KR1020000004631
申请日：2000-01-31
Applicant: 한국과학기술연구원
IPC: C07D473/16
Abstract: PURPOSE: Provided are novel adenine compounds which inhibit the cyclin dependent kinase (CDK), specifically, isopropylpurine derivatives with the substitution at C-2,6,9 positions and their preparation method. These adenine compounds are more effective than existing olomousine and roscovitine in CDK inhibition. CONSTITUTION: The compounds are represented by chemical formula 1, wherein R1 is piperidino, piperazino, pyrrolidino or thiomorpholino group which is substituted by one or more groups selected from hydroxyalkyl amino, hydroxy, hydroxyalkyl, carboxylic acid, aldehyde and oxim group. Most preferably R1 is hydroxyalkylamino or 4-carboxy-2-hydroxymethyl pyrrolidino group. The preparation process includes the steps of: reacting 2,6-dichloropurine with 3-chloroaniline in butanol solution; reacting the resultant compound with isopropyl halide in the presence of strong base and reacting the product, in 4:1 mixed solvent of n-butanol and DMSO, with piperidine, piperazino, pyrrolidino or thiomorpholino group which is substituted by one or more group selected from hydroxyalkyl amino, hydroxy, hydroxyalkyl, carboxylic acid, aldehyde and oxim group.
Abstract translation: 目的：提供抑制细胞周期蛋白依赖性激酶（CDK）的新型腺嘌呤化合物，特别是C-2,6,9位取代的异丙基嘌呤衍生物及其制备方法。 这些腺嘌呤化合物在CDK抑制中比现有的olomousine和roscovitine更有效。 构成：化合物由化学式1表示，其中R 1是被一个或多个选自羟基烷基氨基，羟基，羟基烷基，羧酸，醛和肟基的基团取代的哌啶子基，哌嗪子基，吡咯烷子基或硫代吗啉代基团。 最优选R 1是羟烷基氨基或4-羧基-2-羟甲基吡咯烷子基。 制备方法包括以下步骤：使2,6-二氯嘌呤与3-氯苯胺在丁醇溶液中反应; 使所得化合物与异丙基卤化物在强碱存在下反应，并使产物在正丁醇和DMSO的4:1混合溶剂中与哌啶，哌嗪子基，吡咯烷子基或硫代吗啉代基反应，所述哌啶，哌嗪基，吡咯烷子基或硫代吗啉代基被一个或多个选自 羟基烷基氨基，羟基，羟烷基，羧酸，醛和肟基。
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公开(公告)号：KR1020010073625A
公开(公告)日：2001-08-01
申请号：KR1020000002389
申请日：2000-01-19
Applicant: 한국과학기술연구원
IPC: C07D401/12
Abstract: PURPOSE: An arylpiperazine compound and a producing method thereof are provided. The arylpiperazine compound can label technetium and F-18 with no having disadvantages of prior arts. CONSTITUTION: The arylpiperazine compound is represented by formula (1), in which R is methanesulfonyl, paratoluenesulfonyl or trifluoromethanesulfonyl. A compound of formula (1a) is produced by treating a compound of formula (7) with mesyl chloride under triethylamine. A compounds of formula (1b) is produced by reacting a compound of formula (13) with sodium hydrogen and the compound of formula (7) to produce a compound of formula (14); and dissolving the compound of formula (14) in anhydrous anisole and reacting with anhydrous trifluoro acetic acid, in which the compound of formula (13) is produced by dissolving a compound of formula (9) into trifluoro acetic acid and reacting with triphenylmethanol to produce a compound of formula (10); reacting the compound of formula (10) with triethylamine and bromoacetyl bromide to produce a compound of formula (11); reacting the compound of formula (11) with triphenylmethanol under trifluoro acetic acid to produce a compound of formula (12); and reacting the compound of formula (12) with 3-bromopropionyl chloride. The formula (1b), (9) to (14) are described as in the description.
Abstract translation: 目的：提供芳基哌嗪化合物及其制备方法。 芳基哌嗪化合物可以标记锝和F-18，没有现有技术的缺点。 构成：芳基哌嗪化合物由式（1）表示，其中R是甲磺酰基，对甲苯磺酰基或三氟甲磺酰基。 通过在三乙胺下用甲磺酰氯处理式（7）化合物来制备式（1a）化合物。 通过使式（13）化合物与氢钠和式（7）化合物反应制备式（14）化合物来制备式（1b）化合物; 并将式（14）化合物溶于无水苯甲醚中，与无水三氟乙酸反应，其中式（13）化合物通过将式（9）化合物溶解在三氟乙酸中并与三苯基甲醇反应产生 式（10）的化合物; 使式（10）化合物与三乙胺和溴乙酰溴反应生成式（11）化合物; 在三氟乙酸下使式（11）化合物与三苯基甲醇反应，生成式（12）化合物; 并使式（12）化合物与3-溴丙酰氯反应。 公式（1b），（9）〜（14）在说明书中进行说明。
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公开(公告)号：KR100281827B1
公开(公告)日：2001-04-02
申请号：KR1019980038443
申请日：1998-09-17
Applicant: 한국과학기술연구원
Abstract: 본 발명은 유기 아민의 아실화 방법에 있어서, 아실화제로서 다음 화학식 1을 갖는 N,N-디아실이미다졸론 유도체를 사용하는 아실화 방법을 제공한다:
화학식 1.
식 중에서,
R
1 과 R
2 는 같거나 다르고, 메틸, 에틸 또는 C
3 -C
19 의 직쇄 또는 치환된 알킬기, 페닐, 헤테로 사이클릭 화합물, 알콕시기 및 유기산 치환기로 이루어진 군 중에서 선택되며;
R
3 와 R
4 는 같거나 다르고, 수소 원자, 메틸 또는 에틸, 페닐, 치환된 페닐 및 알콕시카보닐기로 이루어진 군 중에서 선택되거나, R
3 와 R
4 는 이들이 결합되어 있는 탄소 원자와 함께 다음 구조를 갖는 R 치환 벤젠 고리를 형성함
(여기서, R은 수소 원자, 카르복실기 또는 설폰산기임).-
公开(公告)号：KR100154354B1
公开(公告)日：1998-11-16
申请号：KR1019940013194
申请日：1994-06-11
Applicant: 한국과학기술연구원
IPC: C07D487/04 , A61K31/43 , C07D207/00 , C07D477/04
Abstract: 본 발명에서는 다음 일반식(Ⅰ)의 피롤리디닐티오계 카바페넴 유도체가 개시된다.
본 발명의 카바페넴 유도체는 내성균에 효과가 있으며 DHP-1 효소에 대한 안정성이 우수하다.-
Patent Agency Ranking
公开(公告)号：KR1019950014061A
公开(公告)日：1995-06-15
申请号：KR1019930023229
申请日：1993-11-03
Applicant: 한국과학기술연구원
IPC: C07C251/32 , C07C249/08
Abstract: 본 발명은 1단계 또는 2단계 반응에 의한 의학 진단용 시약인 (RR/SS)-4, 8-디아지-3, 6, 6, 9- 테트라 메틸 운데칸-3, 8-디엔-2, 10-디온 비스 옥심의 제조방법에 관한 것이다. 본 발명에 의해 d, 1-HM-PAO가 효과적으로 얻어질 수 있다.
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17.发明授权디플루오로페닐 유도체를 갖는 신규한 옥사졸리디논 유도체또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 항생제 조성물 失效具有二氟苯基衍生物的新型恶唑烷酮衍生物或其药学上可接受的盐，其制备方法和含有其作为活性成分的抗生素药物组合物
公开(公告)号：KR100980681B1
公开(公告)日：2010-09-07
申请号：KR1020080090659
申请日：2008-09-16
Applicant: 한국과학기술연구원
IPC: C07D413/10 , C07D413/02
CPC classification number: C07D413/10
Abstract: 본 발명은 하기 화학식 1로 표시되는 디플루오로페닐 유도체를 갖는 신규한 옥사졸리디논 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 항생제 조성물에 관한 것으로, 본 발명에 따른 조성물에 유효성분으로 함유되는 옥사졸리디논 유도체 및 이의 약학적으로 허용가능함 염은 헤모필루스 인플루엔자(Haemophilus influenza), 비병원성 포도상구균(Coagulase negative staphylococi) 등을 포함하는 그람양성균 및 반코마이신 내성 장내구균(VRE) 등을 포함하는 내성 균주들에 대하여 유의한 항균 활성을 나타내므로, 항생제로서 유용하게 사용될 수 있다.
[화학식 1]
.
(상기 화학식 1에서, R은 본 명세서에서 정의한 바와 같다.)
옥사졸리디논, 리네졸리드, 스피로[2,4]헵탄, MRSA, 반코마이신내성균-
18.发明公开신규2'-데옥시-2'-[18Ｆ]플루오로-5-메틸-1-β-Ｌ-아라비노퓨라노실우라실 화합물, 이의 제조방법 및 이를 포함하는유전자 영상용 조영제 无效新的2'-脱氧-2' - [18 F]氟-5-甲基-1-β-L-阿拉伯呋喃亚磺酰脲化合物，其制备方法及其对照成像用于成像包含其的基因表达
公开(公告)号：KR1020090073659A
公开(公告)日：2009-07-03
申请号：KR1020070141668
申请日：2007-12-31
Applicant: 한국과학기술연구원
IPC: C07D405/04 , C07H15/22
Abstract: A manufacturing method for manufacturing a 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound is provided to produce a compound having high intake rate by specifically activating in a cell line which HSV-TK gene is specifically expressed. A 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound is denoted by the chemical formula 1. A method for manufacturing the 2-deoxy-2-[18F]fluoro-5-methyl-1-beta-L-arabinofuranosyluracil compound comprises: a step of reacting anhydrous trifluoro methanesulfonyl in a compound of the chemical formula 2 under the presence of organic solvent to produce the tribenzoyl triflate saccharide compound of the chemical formula 3; a step of introducing fluorine-18 to produce a compound of the chemical formula 4; a step of reacting the compound of the chemical formula 4 with anhydrous acetic acid under the presence of organic solvent to produce a compound of the chemical formula 5; a step of reacting the compound of the chemical formula 5 with silylated thymine to produce a compound of the chemical formula 7; and a step of hydrolyzing the compound of the chemical formula 7 to produce the compound of the chemical formula 1.
Abstract translation: 提供了制备2-脱氧-2- [18 F]氟-5-甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物的制备方法，通过在细胞系中特异性活化以产生高摄入率的化合物，其中HSV-TK 基因被特异表达。 2-脱氧-2- [18 F]氟-5-甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物由化学式1表示。制备2-脱氧-2- [18 F]氟-5- 甲基-1-β-L-阿拉伯呋喃糖尿嘧啶化合物包括：在有机溶剂的存在下，使化学式2的化合物中的无水三氟甲烷磺酰化反应生成化学式3的三苯甲酰基三氟甲磺酸酯化合物的步骤; 引入氟-18以制备化学式4的化合物的步骤; 在有机溶剂的存在下使化学式4的化合物与无水乙酸反应以产生化学式5的化合物的步骤; 使化学式5的化合物与甲硅烷基化的胸腺嘧啶反应以产生化学式7的化合物的步骤; 以及水解化学式7的化合物以制备化学式1的化合物的步骤。
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公开(公告)号：KR1020050021835A
公开(公告)日：2005-03-07
申请号：KR1020030059624
申请日：2003-08-27
Applicant: 한국과학기술연구원
IPC: A01G31/02
CPC classification number: Y02P60/216
Abstract: PURPOSE: A method of growing bean sprouts with a bean sprout growing apparatus for sterilizing or disinfecting collected cultivation water with a disinfectant, coagulating pollutants or impurities contained in the cultivation water with a coagulant and an coagulant aid and purifying cultivation water with a bottom-up sand filter layer is provided. The bean growing method can recycle the purified cultivation water, thereby reducing production cost and preventing environmental pollution. CONSTITUTION: The bean sprouts growing method consists of: collecting cultivation water containing pollutants or impurities discharged from a bean sprouts cultivation part; sterilizing or disinfecting cultivation water by adding a disinfectant to the collected cultivation water; coagulating the pollutant or impurities by inputting a coagulant and an coagulant aid to the sterilized cultivation water; purifying cultivation water containing coagulated sludge by passing through a sand filter layer(5,6) from the lower part to the upper part; and resupplying the purified cultivation water to the bean sprouts cultivation part. The disinfectant is 0.5 to 5ppm chlorine dioxide. The coagulant is at least one selected from polyaluminum chloride or polyacrylamide and the coagulant aid is at least one selected from clay, loess, kaolin, vermiculite, active carbon, carbonized rice hull, carbonized rice hull ash, quicklime, K2CO3 and KOH.
Abstract translation: 目的：一种用豆芽生长装置种植豆芽的方法，用消毒剂消毒或消毒收集的培养水，用絮凝剂和助凝剂将培养水中含有的污染物或杂质凝结，并用自下而上的方式净化培养水 提供砂滤层。 豆类生长方法可以回收纯化的培养水，从而降低生产成本，防止环境污染。 规定：豆芽生长方法包括：收集含有从豆芽种植部分排出的污染物或杂质的培养水; 通过向收集的培养水中加入消毒剂来消毒或消毒培养水; 通过向灭菌的栽培水输入凝结剂和助凝剂来使污染物或杂质凝结; 通过从下部到上部通过砂过滤层（5,6）来净化含有凝结污泥的培养水; 并将纯化的培养水补给豆芽培养部分。 消毒剂为0.5〜5ppm二氧化氯。 絮凝剂是选自聚氯化铝或聚丙烯酰胺中的至少一种，絮凝剂是选自粘土，黄土，高岭土，蛭石，活性炭，碳化米壳，碳化稻壳灰，生石灰，K 2 CO 3和KOH中的至少一种。
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公开(公告)号：KR100441406B1
公开(公告)日：2004-07-23
申请号：KR1020010054467
申请日：2001-09-05
Applicant: 한국과학기술연구원
IPC: C07D487/02
Abstract: PURPOSE: Antibacterial carbapenem derivatives which are active against resistant strains are provided. They are pyrrolidine thiol carbapenems represented by formula(1), wherein R1 is hydrogen, substituted or unsubstituted lower alkly, heterocycles containing N or S, sulfonyl substituted with lower alkyl, carbonyl substituted with heterocycles containing N or S, benzyl, amide or hydroxy group; R2 is hydrogen, hydroxy alkyl, amide or ester group. CONSTITUTION: The method of preparation comprises: reacting phosphate compound with thiol derivatives represented by formula(2) under base and obtaining protected carbapenem derivatives; de-protecting them using hydrogen and palladium as a catalyst; and purifying with porous resin and freeze drying. In formula (2), R1 and R2 are same as in formula(1) and PNZ is p-nitrobenzyloxycarbonyl group.
Abstract translation: 目的：提供对抗性菌株有活性的抗菌碳青霉烯衍生物。 它们是由式（1）表示的吡咯烷硫醇碳青霉烯类，其中R1是氢，取代或未取代的低级烷基，含有N或S的杂环，被低级烷基取代的磺酰基，被含有N或S的杂环取代的羰基，苄基，酰胺基或羟基 ; R2是氢，羟基烷基，酰胺或酯基。 构成：制备方法包括：使磷酸酯化合物与式（2）所示的硫醇衍生物在碱的作用下反应，得到被保护的碳青霉烯衍生物; 用氢和钯作为催化剂对其进行脱保护; 并用多孔树脂纯化并冷冻干燥。 式（2）中，R 1和R 2与式（1）相同，PNZ是对硝基苄氧基羰基。
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