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公开(公告)号：KR100466797B1
公开(公告)日：2005-01-24
申请号：KR1020010089276
申请日：2001-12-31
Applicant: 한국과학기술연구원
IPC: C07D223/16
Abstract: PURPOSE: Benzoazepine derivatives and a preparation process thereof using indium are provided, thereby rapidly and easily preparing the benzoazepine derivatives using an appropriate amount of indium powder. CONSTITUTION: Benzoazepine derivatives are represented by the formula IV, wherein X is H, F, Cl, Br, I, alkyl or alkoxy. The benzoazepine derivatives represented by the formula III are also provided, wherein R is methyl, ethyl or hydrogen; and X is H, F, Cl, Br, I, alkyl or alkoxy. A process for preparing benzoazepine derivatives of the formula IV comprises the steps of: (1) stirring 2-nitro benzaldehyde derivatives of the formula I and methyl 2-(bromomethyl) acrylate or ethyl 2-(bromomethyl) acrylate in water or aqueous organic solvent, together with indium coil or indium thin layer and acid to prepare a compound of the formula III; and (2) reacting the compound of the formula III with base in an organic solvent, wherein the aqueous organic solvent in the step (1) is tetrahydrofuran solution, acetonitrile solution, N,N-dimethylformamide solution, methylalcohol solution or ethylalcohol solution; the base in the step (2) is sodium hydride, potassium butoxide, sodium bicarbonate, sodium carbonate, potassium carbonate or cesium carbonate; and the organic solvent in the step (2) is tetrahydrofuran, N,N-dimethylformamide, methylsulfoxide, dimethylsulfoxide or dichloromethane.
Abstract translation: 目的：提供苯并氮杂衍生物及其使用铟的制备方法，由此使用适量的铟粉迅速且容易地制备苯并吖庚因衍生物。 构成：苯并氮杂衍生物由式Ⅳ表示，其中X是H，F，Cl，Br，I，烷基或烷氧基。 还提供了由式III表示的苯并吖庚因衍生物，其中R是甲基，乙基或氢; X是H，F，Cl，Br，I，烷基或烷氧基。 制备式Ⅳ的苯并吖庚因衍生物的方法包括以下步骤：（1）将式I的2-硝基苯甲醛衍生物和2-（溴甲基）丙烯酸甲酯或2-（溴甲基）丙烯酸乙酯在水或含水有机溶剂 与铟线圈或铟薄层和酸一起制备式III的化合物; （2）使式III化合物与碱在有机溶剂中反应，其中步骤（1）中的含水有机溶剂为四氢呋喃溶液，乙腈溶液，N，N-二甲基甲酰胺溶液，甲醇溶液或乙醇溶液; 步骤（2）中的碱为氢化钠，丁醇钾，碳酸氢钠，碳酸钠，碳酸钾或碳酸铯; 步骤（2）中的有机溶剂为四氢呋喃，N，N-二甲基甲酰胺，甲基亚砜，二甲基亚砜或二氯甲烷。
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公开(公告)号：KR1020040039033A
公开(公告)日：2004-05-10
申请号：KR1020020066652
申请日：2002-10-30
Applicant: 한국과학기술연구원
IPC: C07C209/32
Abstract: PURPOSE: A method for reducing a nitro compound into an amine compound by using an indium metal wire is provided, to prevent the conglomeration of indium metal and to allow the reduction reaction to be carried out under a milder condition. CONSTITUTION: The method comprises the step of reducing a nitro compound represented by the formula 1 into an amine compound represented by the formula 2 by using an indium metal wire in an aqueous solution, wherein R is an aliphatic or aromatic compound. Preferably the reaction is carried out at a temperature of 20-25 deg.C; and the amount of the indium metal is 1.5-2.0 equivalences per a nitro group. Optionally the reaction is carried out in the presence of HCl or HBr which is added to make the pH of the reaction mixture be 1-2.
Abstract translation: 目的：提供通过使用铟金属线将硝基化合物还原成胺化合物的方法，以防止铟金属的聚集并允许在较温和的条件下进行还原反应。 构成：该方法包括通过在水溶液中使用铟金属线将式1所示的硝基化合物还原成由式2表示的胺化合物的步骤，其中R是脂族或芳族化合物。 反应优选在20-25℃的温度下进行; 并且铟金属的量相对于硝基为1.5-2.0当量。 任选地，反应在HCl或HBr的存在下进行，其加入以使反应混合物的pH为1-2。
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公开(公告)号：KR1020030065890A
公开(公告)日：2003-08-09
申请号：KR1020020005946
申请日：2002-02-01
Applicant: 한국과학기술연구원
IPC: C07D453/02
Abstract: PURPOSE: Provided are Quinuclidine compounds which are useful for treatment of brain-nervous diseases caused by cholinergic neurotransmission such as Alzheimer's disease and a preparation method thereof. CONSTITUTION: A quinuclidine compounds of the formula (I) and pharmaceutically acceptable salts thereof are provided, wherein n is an integer of 1 to 5; R is a substituent on a benzene ring, hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-6 alkyl, 1,2 or 3 fluorine substituted C1-6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-6 alkenyl, 1,2 or 3 fluorine substituted C2-6 alkenyl, C2-6 alkynyl, 1,2 or 3 fluorine substituted C2-6 alkynyl, and C3-7 cycloalkyl. A method for preparing the quinuclidine compounds of the formula (I) comprises reacting a compound of the formula (II) with a compound of the formula (III) or (IV), wherein R1 and R2 are independently C1-6 alkyl, aryl or arylalkyl.
Abstract translation: 目的：提供可用于治疗由胆碱能神经传递如阿尔茨海默病引起的脑神经疾病的奎宁环化合物及其制备方法。 构成：提供式（I）的奎宁环化合物及其药学上可接受的盐，其中n为1至5的整数; R是苯环上的取代基，氢，F，Cl，甲氧基，OH，NH2，NO2,3,4-二甲氧基，2,4-二甲氧基，氰基，C1-6烷基，1,2或3个氟取代的C1 -6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C2-6烯基，1,2或3个氟取代的C2-6烯基，C2-6炔基，1,2或3个氟取代的C2-6炔基，C3-7 环。 制备式（I）的奎宁环化合物的方法包括使式（II）的化合物与式（III）或（IV）的化合物反应，其中R 1和R 2独立地为C 1-6烷基，芳基或 芳。
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公开(公告)号：KR100373485B1
公开(公告)日：2003-02-25
申请号：KR1019990041612
申请日：1999-09-28
Applicant: 한국과학기술연구원
IPC: C07D295/22
Abstract: PURPOSE: Provided is a novel isooxazol piperazin derivative which is used as an antagonist against dopamine-1 receptor related to the central nerve system disorders. CONSTITUTION: A novel isooxazol piperazin derivative represented by the formula (1) is manufactured by reacting secondary amine of the formula (2) with aldehyde of the formula (3) in the presence of NaBh(OAc)3, NaBH3CN, or NaBH4 as a reductant and methylene chloride as a solvent at room temperature for 3-24 hours, preferably 12-14 hours. In the formula (1), n is an integer of between 1 and 4; R1 is a phenyl group at an ortho, meta, or para position substituted by more than one group among halogen, trifluoromethyl, -NO2, alkyl group of C1-C3 , and alkoxy group of C1-C3, or an alkyl group of C1-C3, hydroxy group, 4-(2-keto-1-benzimidazolerynyl), 1-(2-(trifluoromethyl)benzene, 4-(4-chlorophenyl)-4-hydroxy, 1-(2-pyrimidyl), or 1-benzyl group; R2-R5 is hydrogen; R6 is a phenyl group at an ortho, meta, or para position substituted by more than one group among halogen group, trifluoromethyl group , -CN, -NO2, an alkyl group of C1-C3, phenoxy group, and alkoxy group of C1-C3 and an unsaturated 5 or 6 hetero ring group having more than one atom from an alkyl group of C-C3, alkoxy group of C1-C3, thiophenyl group, (2-phenyl)vinyl group, pyridyl group, and from oxygen, sulfur, and nitrogen; and Q is isoxazol (A) or 4,5-dihydroisoxazole derivative (B).
Abstract translation: 用途：提供了一种新的异恶唑哌嗪衍生物，其用作针对与中枢神经系统疾病相关的多巴胺-1受体的拮抗剂。 结构式（1）表示的新型异恶唑哌嗪衍生物是通过使式（2）的仲胺与式（3）的醛在NaBh（OAc）3，NaBH3CN或NaBH4存在下反应制备的 还原剂和二氯甲烷作为溶剂在室温下反应3-24小时，优选12-14小时。 式（1）中，n为1〜4的整数， R 1是在卤素，三氟甲基，-NO 2，C 1 -C 3的烷基和C 1 -C 3的烷氧基中的多于一个基团取代的邻位，间位或对位的苯基，或者C1- C3-羟基，4-（2-酮-1-苯并咪唑基），1-（2-（三氟甲基）苯，4-（4-氯苯基）-4-羟基，1-（2-嘧啶基） 苄基; R 2 -R 5是氢; R 6是在卤素基团，三氟甲基，-CN，-NO 2，C 1 -C 3烷基，C 1 -C 3烷氧基， 苯氧基和C 1 -C 3的烷氧基以及具有超过一个来自C 1 -C 3的烷基，C 1 -C 3的烷氧基，噻吩基，（2-苯基）乙烯基的不饱和5或6个杂环基 ，吡啶基和氧，硫和氮;并且Q是异恶唑（A）或4,5-二氢异恶唑衍生物（B）。
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公开(公告)号：KR100362706B1
公开(公告)日：2002-12-11
申请号：KR1020000021258
申请日：2000-04-21
Applicant: 한국과학기술연구원
IPC: C07C209/32
Abstract: 본 발명은 인듐 금속을 이용하여 니트로기(-NO
2 )를 갖는 화합물을 아민(-NH
2 ) 화합물로 환원시키는 방법을 제공한다. 보다 구체적으로는 인듐 금속을 이용하여 화학식 1을 갖는 지방족 또는 방향족 화합물을 화학식 2의 화합물로 환원시키는 방법을 제공한다.
[화학식 1]
[화학식 2]
상기 화학식 1 및 2에서, R은 지방족 또는 방향족 화합물을 나타내며, n은 1-5의 정수, 바람직하게는 1-3의 정수, 가장 바람직하게는 1 또는 2이다.
인듐 금속을 이용한 본 발명의 환원 반응은 상온에서 짧은 시간 내에 진행될 뿐만 아니라 수개의 니트로기를 짧은 시간 내에 한번에 환원시킬 수 있다. 또한 분자내 다른 관능기에 영향을 미치지 아니하고 니트로기만 선택적으로 환원시킬 수 있으며, 수용액 상에서 반응이 쉽게 진행되므로 환경친화적 산업 공정이다는 장점을 가지고 있다. 따라서 화학 공업 분야에서 다양하게 응용될 수 있다.-
Patent Agency Ranking
公开(公告)号：KR100309704B1
公开(公告)日：2001-09-29
申请号：KR1019990016355
申请日：1999-05-07
Applicant: 한국과학기술연구원
IPC: C07D499/00
CPC classification number: Y02P20/55
Abstract: 일반식(I')로표시되는 7-옥소세팔로스포린유도체를일반식(II)으로표시되는알릴할라이드또는일반식(III)으로표시되는아세틸렌할라이드와인듐또는아연금속존재하에용매와함께반응시켜신규한일반식(I)로표시되는세펨유도체및 이의제조방법에관한것으로, 이는베타-락타마제저해제및 항생제제조의중요한중간체로사용된다
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公开(公告)号：KR100299044B1
公开(公告)日：2001-09-22
申请号：KR1019990001300
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D501/04
Abstract: 일반식(II)의 3-치환세팔로스포린유도체를인듐금속원자또는인듐화합물존재하에반응시켜일반식(I)의 7-아미노데스아세톡시세팔로스포린산유도체와일반식(III)의 3-엑소메틸렌세펨유도체와의혼합물을얻고이 혼합물중의일반식(III)의 3-엑소메틸렌세펨유도체를일반식(I)의 7-아미노데스아세톡시세팔로스포린산유도체로전이시키는제조방법에관한것이다.
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公开(公告)号：KR1020010084202A
公开(公告)日：2001-09-06
申请号：KR1020000009065
申请日：2000-02-24
Applicant: 한국과학기술연구원
IPC: C07D501/16
CPC classification number: Y02P20/55
Abstract: PURPOSE: Provided is a cephem derivative which has broad range of antimicrobial activity. And its producing method is also provided. CONSTITUTION: The cephalosporin compounds represented by formula (1) and its pharmaceutically acceptable salts are produced. In the formula, R1 is hydrogen or an amine protecting group generally used in cephalosporin compounds; R2 is hydrogen or an oxim protecting group; R3 is hydrogen or a chloro group; R5 is hydrogen or an ester producing group, a salt producing atom or a carboxy protecting group; and R4 is ring substituent having Q group, in which Q is hydrogen, halogen, hydroxy, mercapto, cyano, carboxy, carboxylic acid ester, carbamoyloxymethyl, N,N-dimethylcarbamoyloxymethyl, carbamoyl, N,N-dimethylcarbamoyl, C1 to C4 alkyl, C1 to C4 alkyloxy, halogen substituted methyl, halogen substituted C1 to C4 alkyloxy, aryl or hetero ring substituent. The cephalosporin derivative of formula (1) is produced by reacting a compound of formula (7) with a compound of formula (8).
Abstract translation: 目的：提供具有广泛抗菌活性的头孢烯衍生物。 并提供其生产方法。 构成：制备由式（1）表示的头孢菌素化合物及其药学上可接受的盐。 式中R1是氢或通常用于头孢菌素化合物的胺保护基; R2是氢或肟基保护基; R3是氢或氯基; R5是氢或产酯基，产盐原子或羧基保护基; R4是具有Q基团的环取代基，其中Q是氢，卤素，羟基，巯基，氰基，羧基，羧酸酯，氨基甲酰氧基甲基，N，N-二甲基氨基甲酰氧基甲基，氨基甲酰基，N，N-二甲基氨基甲酰基， C1至C4烷氧基，卤素取代的甲基，卤素取代的C1至C4烷氧基，芳基或杂环取代基。 式（1）的头孢菌素衍生物通过使式（7）的化合物与式（8）的化合物反应来制备。
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公开(公告)号：KR1020000073205A
公开(公告)日：2000-12-05
申请号：KR1019990016355
申请日：1999-05-07
Applicant: 한국과학기술연구원
IPC: C07D499/00
CPC classification number: Y02P20/55
Abstract: PURPOSE: A cephem derivative using indium and zinc and a preparation method thereof are provided. The cephem derivative is used as an intermediate in manufacturing beta-lactamase inhibiting agent and antibiotics CONSTITUTION: Cephem derivative as represented by formula(I) is prepared by reacting 7-oxo cephalosporin derivative as represented by formula(I'), allyl halide as represented by formula(II), acetylene halide as represented by formula(III), solvent in the presence of indium or zinc. In the formula (I): R1 is allyl derivative or acetylene derivative; R2 is hydrogen, carboxylic acid salt(sodium salt and potassium salt as inorganic salt, alkyl amine salt, aromatic amine salt as organic salt) or carboxy protecting group(4-methoxybenzyl, diphenylmethyl, 4-nitrobenzyl and useful thing as protecting group of molecule in penicillin or cephalosporin compound field); R3 is hydrogen, halogen, hydroxy or acetoxy group; and R4,R5,R6 are each hydrogen, methyl, ethyl, carboxylic acid or ester.
Abstract translation: 目的：提供使用铟和锌的头孢烯衍生物及其制备方法。 头孢衍生物用作制造β-内酰胺酶抑制剂和抗生素的中间体构成：由式（I）表示的头孢烯衍生物通过如表达的式（I'）表示的7-氧代头孢菌素衍生物，烯丙基卤化物 由式（II）表示的式（III）所示的炔酰卤，在铟或锌存在下的溶剂。 在式（I）中：R 1是烯丙基衍生物或乙炔衍生物; R2是氢，羧酸盐（钠盐和钾盐作为无机盐，烷基胺盐，作为有机盐的芳族胺盐）或羧基保护基（4-甲氧基苄基，二苯基甲基，4-硝基苄基和有用的物质作为分子保护基 在青霉素或头孢菌素化合物领域）; R3是氢，卤素，羟基或乙酰氧基; 并且R 4，R 5，R 6各自为氢，甲基，乙基，羧酸或酯。
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公开(公告)号：KR1019990068967A
公开(公告)日：1999-09-06
申请号：KR1019980002915
申请日：1998-02-03
Applicant: 한국과학기술연구원
IPC: C07D501/24
Abstract: 본 발명은 신규한 일반식(I)로 표시되는 (E)-프로페닐 4급 암모늄 세펨 화합물과 그의 약제학적으로 허용되는 염 및 이의 제조 방법에 관한 것이다. 본 발명에서 제조된 화합물들은 그람 양성균이나 그람 음성균에 대해 우수한 항균력을 나타내므로 세팔로스포린 계열 의약품에 유용하게 사용될 수 있다.
일반식(I)에 있어서, R
1 은 수소 또는 아민보호기를 표시하며, R
2 는 수소, 메틸, 2-플루오르에틸 또는 옥심보호기를 표시하며, R
3 는 수소, 카르복실산염 형성기 또는 카르복실 보호기를 표시하며, R
4 는 메톡시, 치환체를 가진 카바모일, 옥사디아졸 또는 트리아졸로 표시되는 5환 헤테로고리 치환체를 표시하며, n은 1 또는 2를 표시한다.
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