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公开(公告)号：KR1020030058742A
公开(公告)日：2003-07-07
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快速且容易地制备苯并氮杂衍生物。 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表示的苯并氮杂衍生物，其中R是甲基，乙基或氢; 且X为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中搅拌 ，与铟线圈或铟薄层和酸一起制备式III化合物; 和（2）使式III化合物与碱在有机溶剂中反应，其中步骤（1）中的有机有机溶剂是四氢呋喃溶液，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; 并且步骤（2）中的有机溶剂是四氢呋喃，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：KR1020030058741A
公开(公告)日：2003-07-07
申请号：KR1020010089275
申请日：2001-12-31
Applicant: 한국과학기술연구원
IPC: C07D209/36
Abstract: PURPOSE: Indol derivatives and a preparation process thereof are provided, thereby rapidly preparing indol derivatives under mild conditions in higher yield. CONSTITUTION: Indol derivatives are represented by the formula 6, wherein R is H, or halogen selected from Cl, F, Br and I; and Y is -Ts(tosyl), -Ms(mesyl) or -Ac(acetyl). A process for preparing the indol derivatives of the formula 6 comprises the steps of: reacting a compound of the formula 1 with a compound of the formula 2 in the presence of indium metal and acid to simultaneously perform allylation of aldehyde and reduction of nitro group, thereby preparing a compound of the formula 3; protecting amine group of the compound of the formula 3 to prepare a compound of the formula 4; oxidizing secondary alcohol of the compound of the formula 4 to prepare a compound of the formula 5; and cyclization of the compound of the formula 5 in the presence of organic base, wherein the oxidation of secondary alcohol uses pyridinium chlorochromate(PCC) or pyridinium dichromate(PDC) or Swern's oxidation or Dess-Martin periodinane oxidation; and the organic base is diisopropylethylamine, DBU (1,8-diazabicyclo£5.4.0|undec-7-ene), DBN (1,5-diazabicyclo£4.3.0|non-5-ene), triethylamine or pyridine.
Abstract translation: 目的：提供吲哚衍生物及其制备方法，从而在温和条件下以更高的收率快速制备吲哚衍生物。 构成：吲哚衍生物由式6表示，其中R是H，或选自Cl，F，Br和I的卤素; 和Y是-T（甲苯磺酰基），-Ms（甲磺酰）或-Ac（乙酰基）。 制备式6的吲哚衍生物的方法包括以下步骤：在铟金属和酸的存在下使式1的化合物与式2的化合物反应，以同时进行醛的还原和烯基的还原， 从而制备式3的化合物; 保护式3化合物的胺基以制备式4的化合物; 氧化式4化合物的仲醇制备式5的化合物; 在有机碱的存在下环化式5的化合物，其中仲醇的氧化使用氯铬酸吡啶鎓（PCC）或重铬酸吡啶鎓（PDC）或Swern的氧化或Dess-Martin氧化氧化; 有机碱是二异丙基乙胺，DBU（1,8-二氮杂双环{5.4.0 |十一-7-烯），DBN（1,5-二氮杂双环{4.3.0 |非-5-烯），三乙胺或吡啶。
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133.发明公开
公开(公告)号：KR1020030056992A
公开(公告)日：2003-07-04
申请号：KR1020010087362
申请日：2001-12-28
Applicant: 한국과학기술연구원
IPC: C07D209/48
CPC classification number: C07D209/48
Abstract: PURPOSE: Carbonyl compounds and a preparation process thereof using carbonyl reductase isolated from Kluyveromyces marxianus are provided. The carbonyl compounds are useful as intermediates for preparing beta-lactam family antimicrobial agents. CONSTITUTION: Carbonyl compounds represented by the formula(Ia) and (Ib) are provided, wherein R is methyl, ethyl, propyl, isopropyl, isobutyl and allyl containing saturated or unsaturated alkyl, or phenyl containing aryl; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, halogen atoms including Br, Cl, F and I, methyl and ethyl containing C1-C4 alkyl, hydroxy, C1-C4 alkoxy, acetoxy containing ester, and phenyl. A process for preparing the carbonyl compound of the formula(Ia) and (Ib) comprises the steps of: mixing a compound of formula(VI) with β-NADPH and a pH 5.0 to 8.0 buffer solution; adding carbonyl reductase isolated from Kluyveromyces marxianus into the mixture; and reacting the mixture at 20 to 40 deg. C for 5 hours to 5 days.
Abstract translation: 目的：提供羰基化合物及其使用从马克斯克鲁维酵母分离的羰基还原酶的制备方法。 羰基化合物可用作制备β-内酰胺家族抗微生物剂的中间体。 构成：提供由式（Ia）和（Ib）表示的羰基化合物，其中R是含有饱和或不饱和的烷基或含苯基的芳基的甲基，乙基，丙基，异丙基，异丁基和烯丙基; R 1，R 2，R 3和R 4独立地选自氢，包括Br，Cl，F和I的卤素原子，含有C 1 -C 4烷基，羟基，C 1 -C 4烷氧基，含乙酰氧基的酯和苯基的甲基和乙基 。 制备式（Ia）和（Ib）的羰基化合物的方法包括以下步骤：将式（VI）化合物与β-NADPH和pH 5.0-8.0缓冲溶液混合; 将从马克斯克鲁维酵母分离的羰基还原酶加入到混合物中; 并使混合物在20至40℃下反应。 C为5小时至5天。
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公开(公告)号：KR1020000067451A
公开(公告)日：2000-11-15
申请号：KR1019990015261
申请日：1999-04-28
Applicant: 한국과학기술연구원
IPC: C07D501/22
CPC classification number: Y02P20/55
Abstract: PURPOSE: Cepham derivatives prepared by the reaction of 3-hydroxy cephem derivatives and allylhalide or acetylene halide in a solvent in the presence of a metal catalyst and process for the preparation method thereof are provided which can be used as an intermediate for the manufacture of cephem antibiotics. CONSTITUTION: Cepham derivatives of formula (I) useful as an intermediate for producing cephem antibiotics are prepared by the reaction of 3-hydroxy cephem derivatives of formula (V) and allylhalide (III) or acetylene halide in a solvent in the presence of a metal catalyst at 0 to 100°C for 1 to 96 hr. In formula, R1 represents phenylacetyl, 2-£2-amino(1,3-thiazole-4-yl)-2-(hydroxyalkoxyimino)ethinyl, 2-£2-amino(1,3-thiazole-4-yl)-2-(alkoxyimino)ethinyl or 4-hydroxyphenylglycine derivative, R2 is H, carboxylic acid salts (sodium and potassium salt as inorganic salts, alkylamine salt, aromatic amine salt as organic salts), a molecular protecting group in the cephalosporin field of 4-methoxybenzyl, diphenylbenzyl, diphenylmethyl, 4-nitrobenzyl, allyl as a carboxyl protecting group, in a Q compound, R3, R4 and R5 represent each H, halogen, methyl, ethyl, hydroxy, phenyl or alkoxycarbonyl.
Abstract translation: 目的：提供在金属催化剂存在下，通过3-羟基头孢烯衍生物和烯丙基卤或乙炔卤化物在溶剂中反应制备的Cepham衍生物，其制备方法可用作中间体，用于制备头孢烯 抗生素。 构成：通过式（Ⅴ）的3-羟基头孢烯衍生物与烯丙基卤（III）或炔酰卤在溶剂中在金属存在下的反应制备用作产生头孢类抗生素的中间体的式（I）的头孢类衍生物 催化剂在0〜100℃下反应1〜96小时。 在式中，R 1表示苯乙酰基，2- {2-氨基（1,3-噻唑-4-基）-2-（羟基烷氧基亚氨基）乙炔基，2-（2-氨基（1,3-噻唑-4-基） 2-（烷氧基亚氨基）乙炔基或4-羟基苯基甘氨酸衍生物，R2是H，羧酸盐（作为无机盐的钠盐和钾盐，烷基胺盐，作为有机盐的芳族胺盐），四氢呋喃的头孢菌素领域中的分子保护基， 甲氧基苄基，二苯基苄基，二苯基甲基，4-硝基苄基，烯丙基作为羧基保护基，在Q化合物中，R 3，R 4和R 5各自表示H，卤素，甲基，乙基，羟基，苯基或烷氧基羰基。
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公开(公告)号：KR100267260B1
公开(公告)日：2000-11-01
申请号：KR1019980027115
申请日：1998-07-06
Applicant: 한국과학기술연구원
IPC: C07D501/24 , C07D501/20
Abstract: 본 발명은 경구 투여가 가능한 새로운 세펨 에스테르 화합물 및 이의 제조방법에 관한 것으로, 그램 양성균과 그램 음성균에 대해 광범위의 항균력을 나타내며, 특히 MRSA를 포함한 여러 내성균에 강한 항균력을 나타내는 약제학적으로 유용한 화합물이다.
(I)
일반식 (I)에 있어서, R
1 은 수소 또는 트리틸기를 표시하며, R
2 는 수소, 트리틸기, 메틸기 또는 시클로펜틸기를 표시하며, R
3 는 수소, 클로로, 브로모 또는 메톡시기를 표시하며, R
4 는 아세톡시에틸, 피발로일옥시메틸 또는 이소프로폭시카르보닐옥시에틸기를 표시한다.-
Patent Agency Ranking
公开(公告)号：KR1020000002400A
公开(公告)日：2000-01-15
申请号：KR1019980023118
申请日：1998-06-19
Applicant: 한국과학기술연구원
IPC: C07D453/00 , C07D261/20
Abstract: PURPOSE: The compound is provided which exhibits a high affinity for muscarinic acetylcholine receptor and is useful as therapeutic agent of cerebral nerve disease such as Alzheimer's disease. CONSTITUTION: The carbonyl compound of the formula (II), wherein, n is integer 1 or 2, is reacted with phosphonium salt compound of formula (III), in which R is H, halo, alkoxy, cyano, alkyl, alkenyl, alkinyl, hydroxy, amino, nitro, 4-methoxybenzyloxy, t-butoxycarbonylamino or its salt; R1, R2 and R3 are alkyl, aryl or aralkyl, respectively; X is halogen, or with phosphonate compound of the formula (IV) in the presence of solvent and base to give £(aryl) isooxozolyl| methylene-azabicyclo compound of the formula (I). Thus, 188mg of potassium t-butoxide and 482mg of diethyl 3-(4-methylphenyl)-5-isooxazolylmethylphosphonate being dissolved in tetrahydrofuran are stirred for 30 minutes at 22°C to give 3-£3-(4-methylphenyl)isooxazol-5-yl|methylene-1-azabicyclo£2.2.2|octane oxalic acid salt.
Abstract translation: 目的：提供对毒蕈碱性乙酰胆碱受体具有高亲和力的化合物，并且可用作脑神经疾病如阿尔茨海默病的治疗剂。 构成：其中n为1或2的式（II）的羰基化合物与式（III）的鏻盐化合物反应，其中R为H，卤素，烷氧基，氰基，烷基，烯基，炔基 ，羟基，氨基，硝基，4-甲氧基苄氧基，叔丁氧基羰基氨基或其盐; R1，R2和R3分别是烷基，芳基或芳烷基; X为卤素，或与式（IV）的膦酸酯化合物在溶剂和碱存在下反应，得到（芳基）异恶唑基| 式（I）的亚甲基 - 氮杂二环化合物。 因此，将188mg叔丁醇钾和482mg 3-（4-甲基苯基）-5-异恶唑甲基膦酸二乙酯溶于四氢呋喃中，在22℃下搅拌30分钟，得到3- {3-（4-甲基苯基）异恶唑-4-基） 5-基|亚甲基-1-氮杂双环{2.2.2 |辛酸草酸盐。
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公开(公告)号：KR100215551B1
公开(公告)日：1999-08-16
申请号：KR1019970015200
申请日：1997-04-23
Applicant: 한국과학기술연구원 , 학교법인 중앙대학교 , 한미사이언스 주식회사
IPC: C07D499/87
Abstract: 일반식(Iv)로 표시되는 알데히드와 일반식(Ⅲ)으로 표시되는 아민화합물올 용매존재하에 축합반응시켜 중간체인 일반식(V)의 이민화합물을 제조하고, 일반식(V)로 표시되는 이민화합물의 C-3 위치의 보호기인 R
3 를 제거하여 신규한 일반식(I)로 표시되는 2-베타-이민-페남유도체를 제조하는 것으로 일반식(I)은 이성체를 포합한다. 일반식(I)의 화합물은 베타락타마제 제해제로서 기존의 항생제와 일정 비율로 병용하면 항균작용을 증진시키는 유용한 화합물이다.
상기 일반식들에 있어서, Q는 수소, 메틸, 시아노메틸, 카르복시메틸, 알콕시카르보닐메틸, 디히드록시 벤질유도체, 알릴, 아세 틸유도체, 아미 도알콕시메틸,2-카르복시에톡시유도체, 플루오르알콕시유도체, 피리듐아세틸유도체를 나타내며, R3는 수소, 카르복실산 염, 카르복시 보호기로는 4-메톡시벤질, 디페닐메틸,4-니트로벤질 그리고 알릴 등의 페니실린이나 세팔로스포린 화합물 분야에서 분자의 보호기로 유용한 것을 나타내고, n은 0 ∼ 2의 정수이다.-
公开(公告)号：KR1019960022537A
公开(公告)日：1996-07-18
申请号：KR1019940035869
申请日：1994-12-22
Applicant: 한국과학기술연구원
IPC: C07D501/36 , C07D501/24
Abstract: 본 발명은 하기 일반식(I)의 화합물 또는 그의 제약학적으로 허용되는 염 및 에스테르를 제공한다.
상기 식 중, R
1 은 수소 또는 아미노 보호기이고, R
2 는 수소, 카르복실산 에스테르 또는 카르복실산염 형성기, 또는 카르복시 보호기이거나, 또는 -COOR
2 는 -COO
를 나타내고, R
3 및 R
4 는 서로 동일하거나 상이한 것으로서, 각각 수소 또는 페놀성 히드록시 보호기이고, Q는 수소, 할로겐, C
2-4 알케닐, 할로-C
1-4 알킬, C
3-12 알카노일옥시알킬 또는 Q′-C
1-4 알킬-(여기서, Q′는 헤테로 원자로서 1개 이상의 질소 원자를 함유하고 황원자를 통해 C
1-4 알킬과 결합되는 5원 내지 6월 헤테로 고리임)이다.
또한, 본 발명은 상기 일반식(I)의 화합물의 제조 방법 및 이에 사용되는 중간제의 제조 방법도 제공한다.-
公开(公告)号：KR1020160103390A
公开(公告)日：2016-09-01
申请号：KR1020150025825
申请日：2015-02-24
Applicant: 한국과학기술연구원
IPC: C07D403/04 , C07D249/04 , A61K31/4192
CPC classification number: C07D403/04 , A61K31/4192 , C07D249/04
Abstract: 본발명은미토콘드리아의기능을조절하여신경보호제로서의약효활성을보이면서동시에사이토크롬 P450 이소자임의활성이저하되어독성을유발하는약물과병용투여시에약물의독성을감소시키는 4-(2-벤질옥시페닐)-1-(피롤리딘-3-일)-1,2,3-트리아졸화합물과, 상기화합물의제조방법, 그리고상기화합물을포함하는약제조성물에관한것이다.
Abstract translation: 本发明涉及一种4-（2-苄氧基苯基）-1-（吡咯烷-3-基）-1,2,3-三唑化合物及其制备方法以及包含该化合物的药物组合物。 更具体地，4-（2-苄氧基苯基）-1-（吡咯烷-3-基）-1,2,3-三唑化合物通过调节线粒体的功能而显示出作为神经保护剂的药用活性，并降低药物的毒性 当通过降解细胞色素P450同功酶的活性而给药引起毒性的药物时。
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公开(公告)号：KR101579496B1
公开(公告)日：2015-12-23
申请号：KR1020140083249
申请日：2014-07-03
Applicant: 한국과학기술연구원
CPC classification number: A61K51/0455 , Y10S514/903
Abstract: 본발명은방사성표지된 [C]퀴놀린화합물이포함된방사성조성물에관한것이다. 본발명의 [C]퀴놀린화합물은 mGluR5에대하여특이적으로결합결합하는방사성리간드로유용하므로, mGluR5의과다발현으로유래된질환의진행또는완화를모니터링하기위한영상화제로유용하다.
Abstract translation: 本发明涉及包含放射性标记的喹啉化合物[^ 11C]的放射性组合物。 本发明的喹诺酮化合物[^ 11C]可用作与mGluR5特异性结合的放射性配体，可用作进行或缓解来自mGluR5的过表达的疾病的显像剂。
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