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公开(公告)号：KR1020060024275A
公开(公告)日：2006-03-16
申请号：KR1020040073177
申请日：2004-09-13
Applicant: 한국과학기술연구원
IPC: C07D307/28
Abstract: 본 발명은 입체선택성이 높은 테트라하이드로퓨란 고리화합물과 이의 제조방법에 관한 것으로서, 트리메틸실라닐페타인올을 출발물질로 하고 루이스산(Lewis acid) 촉매를 이용한 분자간 프린스 고리화 반응을 수행하여 알렌(allene)을 포함하고 있는 입체선택성이 높은 다음 화학식 1로 표시되는 신규의 테트라하이드로퓨란 고리화합물과 이 화합물의 제조방법에 관한 것이다.
상기 화학식 1에서, R
1 은 탄소수 1 내지 8의 알킬기, 또는 방향족기를 나타내고, R
2 및 R
3 는 각각 수소원자, 탄소수 1 내지 8의 알킬기, 또는 방향족기를 나타내고, 상기 R
2 및 R
3 는 서로 결합하여 5 내지 7각형의 고리를 형성한다.
입체선택성, 테트라하이드로퓨란, 트리메틸실라닐페타인올, 알렌(allene), 루이스산 촉매, 분자간 프린스 고리화-
公开(公告)号：KR100530345B1
公开(公告)日：2005-11-22
申请号：KR1020020066652
申请日：2002-10-30
Applicant: 한국과학기술연구원
IPC: C07C209/32
Abstract: 본 발명은 인듐 금속 와이어를 사용하여 아래의 화학식 1로 표시되는 니트로 화합물을 상온 및 수용액 중에서 화학식 2로 표시되는 아민 화합물로 환원시키는 방법에 관한 것으로서, 식 중, R은 지방족 또는 방향족 화합물을 나타낸다.
[화학식 1]
[화학식 2]-
公开(公告)号：KR1020040083677A
公开(公告)日：2004-10-06
申请号：KR1020030018239
申请日：2003-03-24
Applicant: 한국과학기술연구원
IPC: C07C17/272
Abstract: PURPOSE: Provided is a method for preparing various types of 2-halo-1,3-diene compounds from allenol with ease by a simple process using no catalyst at a high yield. CONSTITUTION: The method for preparing a 2-halo-1,3-diene represented by formula 3 from an allenol represented by formula 2 comprises treating the allenol with an indium(III) halide salt represented by the formula of InX3 (wherein X is Cl, Br or I), through the reaction route as depicted in the following formula 4. In formulas 2 to 4, each of R1 to R4 represents H, Si, a halogen atom, an alkyl group, an aromatic substituent or a cyclic substituent. In the method, the reaction solvent is selected from acetonitrile and benzene.
Abstract translation: 目的：提供一种通过简单的方法，以高收率使用不含催化剂的方法从丙烯醇制备各种类型的2-卤代-1,3-二烯化合物。 构成：由式2由式2表示的联苯酚制备由式3表示的2-卤代-1,3-二烯的方法包括用式InX 3（其中X为Cl）表示的卤化铟（III）处理三烯酚 ，Br或I）通过如下式4所示的反应路线。在式2至4中，R 1至R 4各自表示H，Si，卤素原子，烷基，芳族取代基或环状取代基。 在该方法中，反应溶剂选自乙腈和苯。
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公开(公告)号：KR100451413B1
公开(公告)日：2004-10-06
申请号：KR1020010087362
申请日：2001-12-28
Applicant: 한국과학기술연구원
IPC: C07D209/48
CPC classification number: C07D209/48
Abstract: A compound represented by a general formula (Ia) or (Ib) and a stereo-selective preparation method thereof using a carbonyl reductase which is separated from Kluyveromyces marxianus. The compound can be prepared by reduction of substituted beta-keto ester and can be used as an intermediate in preparing beta-lactam group antibiotics.
Abstract translation: 由通式（Ia）或（Ib）表示的化合物及其立体选择性制备方法，其使用从马克斯克鲁维酵母分离的羰基还原酶。 该化合物可以通过还原取代的β-酮酯来制备，并且可以用作制备β-内酰胺类抗生素的中间体。
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公开(公告)号：KR100448002B1
公开(公告)日：2004-09-13
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：提供用于治疗由胆碱能神经传递引起的脑神经疾病如阿尔茨海默氏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是1至5的整数; R为苯环上的取代基，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炔基和C3-7 环。 用于制备式（I）奎宁环化合物的方法包括使式（II）化合物与式（III）或（IV）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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Patent Agency Ranking
公开(公告)号：KR100418915B1
公开(公告)日：2004-02-14
申请号：KR1020000071399
申请日：2000-11-28
Applicant: 한국과학기술연구원
IPC: C07D401/04
Abstract: PURPOSE: A 4-aminopiperidine analogue and a producing method thereof are provided, therefore the compound can be useful as a ligand of a muscarine receptor, and it is thus used in study on Alzheimer disease. CONSTITUTION: The 4-aminopiperidine analogue is represented by formula(I), wherein R1, R2, R3, R4, R5, R6 and R7 are hydrogen, cycloalkyl having carbon number of 1 to 6, alkoxy, halogen, hydroxy, hydroxymethyl, aryl, heteroaryl, amino, alkylamino, alkenyl, carbonyl or hetero ring having carbon number of 5 to 7 wherein aryl is a ring having 6 atoms, two rings having 10 atoms or a stable resonance form having double bond to adjacent carbon; heteroaryl is a single ring aromatic group having carbon number of 5 to 6 or a double ring aromatic group having carbon number of 10 in which the heteroaryl has at least one hetero atom of N, O or S; hetero ring consists of 5 to 7 atoms having 1 to 3 of N, O or S; X is carbon or sulfur; and n is an integer of 1 to 2 wherein n is 1 when X is carbon and is 2 when X is sulfur. The 4-aminopiperidine analogue is produced by reacting piperidine or amine(II) with piperazine with ketone(III) in the presence of 1 to 3 equivalent of acetic acid, 2 to 10 equivalent of reducing agent and solvent at room temperature for 3 to 24 hours to produce 4-aminopiperidine(I) and adding NaHCO3 solution and organic solvent to 4-aminopiperidine(I); and drying the extracted 4-aminopiperidine(I), dissolving it, adding 1 to 10 equivalent of hydrogen chloride to the solution, and separating, washing and drying the hydrochloride of 4-aminopiperidine.
Abstract translation: 目的：提供了4-氨基哌啶类似物及其生产方法，因此该化合物可用作毒蕈碱受体的配体，因此用于研究阿尔茨海默病。 构成：4-氨基哌啶类似物由式（I）表示，其中R1，R2，R3，R4，R5，R6和R7是氢，碳数为1-6的环烷基，烷氧基，卤素，羟基，羟甲基，芳基 杂芳基，氨基，烷基氨基，链烯基，羰基或杂环，其中芳基是具有6个原子的环，具有10个原子的两个环或具有与相邻碳双键的稳定的共振形式; 杂芳基为碳数为5至6的单环芳族基团或碳数为10的双环芳族基团，其中杂芳基具有至少一个N，O或S的杂原子; 杂环由5至7个具有1至3个N，O或S的原子组成; X是碳或硫; 并且n是1至2的整数，其中当X是碳时，n是1，当X是硫时，n是2。 4-氨基哌啶类似物是通过使哌啶或胺（II）与哌嗪与酮（III）在1至3当量乙酸，2至10当量还原剂和溶剂的存在下在室温下反应3至24 小时以产生4-氨基哌啶（I）并将NaHCO 3溶液和有机溶剂加入到4-氨基哌啶（I）中; 干燥提取的4-氨基哌啶（I），溶解，加入1至10当量的氯化氢至溶液中，分离，洗涤并干燥4-氨基哌啶的盐酸盐。
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27.发明授权도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 失效도파민D3및D4체택적택적택적규규,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5-규규규규규규규규규규규규규규규규규규규규
公开(公告)号：KR100394083B1
公开(公告)日：2003-08-06
申请号：KR1020000073122
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08
Abstract: The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent,wherein R1, R2, X and n are the same as defined in the specification.
Abstract translation: 本发明涉及对下式（1）所示的多巴胺D3和D4受体具有选择性生物活性的4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下通过还原胺化反应的制备方法，其中R1，R2， X和n与说明书中定义的相同。
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公开(公告)号：KR1020030063853A
公开(公告)日：2003-07-31
申请号：KR1020020004199
申请日：2002-01-24
Applicant: 한국과학기술연구원
IPC: C07D453/02 , C07D471/08 , C07D261/06
Abstract: PURPOSE: An alkenyl azabicyclic compound and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders. CONSTITUTION: An alkenyl azabicyclic compound represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; and R is selected from the group consisting of hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-C6 alkyl, 1, 2 or 3 fluorine substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine substituted C2-C6 alkynyl and C3-C7 cyloalkyl. A method for preparing the alkenyl azabicyclic compound of the formula(I) comprises a compound of the formula(II) with a compound of the formula(III) or formula(IV), wherein R1, R2 and R3 are independently C1-C6 alkyl, aryl or arylalkyl.
Abstract translation: 目的：提供一种烯基氮杂双环化合物及其制备方法，其可用于治疗由胆碱神经传递障碍引起的脑神经疾病。 构成：提供由式（I）表示的烯基氮杂双环化合物及其药学上可接受的盐，其中n为1或2; 并且R选自氢，F，Cl，甲氧基，OH，NH 2，NO 2，3,4-二甲氧基，2,4-二甲氧基，氰基，C 1 -C 6烷基，1,2或3个氟取代的C 1 C 1-6烷基，4-甲氧基苄氧基，叔丁氧基羰基，C 2 -C 6烯基，1,2或3个氟取代的C 2 -C 6炔基和C 3 -C 7环烷基。 制备式（I）的烯基氮杂双环化合物的方法包括式（II）化合物与式（III）或式（IV）化合物，其中R 1，R 2和R 3独立地为C 1 -C 6烷基 ，芳基或芳烷基。
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公开(公告)号：KR1020000073204A
公开(公告)日：2000-12-05
申请号：KR1019990016354
申请日：1999-05-07
Applicant: 한국과학기술연구원
IPC: C07D499/00
CPC classification number: Y02P20/55
Abstract: PURPOSE: A new penam derivative using indium and zinc and a preparation method thereof are provided CONSTITUTION: A novel penam derivative represented by formula(I) is prepared by reacting 6-oxopenam of the formula(I') with ally halide of the formula (II) or acetylene halide of the formula (III) in the presence of indium or zinc. In the formula(I): R1 is allyl derivative and 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-methoxy benzyl, diphenylmethyl, 4-nitrobenzyl, useful thing as protecting group of molecule in penicillin or cephalosporin compound field); R3 is hydrogen, halogen, hydroxy, acetoxy group.
Abstract translation: 目的：提供使用铟和锌的新的penam衍生物及其制备方法构成：式（I）表示的新型penam衍生物通过式（I'）的6-氧代青霉素与式（I'）的式 II）或式（III）的炔酰卤在铟或锌的存在下进行。 在式（I）中：R 1是烯丙基衍生物和乙炔衍生物; R2为氢，羧酸盐（钠盐和钾盐为无机盐，烷基胺盐，芳族胺盐为有机盐）或羧基保护基（4-甲氧基苄基，二苯基甲基，4-硝基苄基，有用物质为保护基 分子在青霉素或头孢菌素化合物领域）; R3是氢，卤素，羟基，乙酰氧基。
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公开(公告)号：KR100181262B1
公开(公告)日：1999-03-20
申请号：KR1019970013988
申请日：1997-04-16
Applicant: 한국과학기술연구원
IPC: C07D501/57
Abstract: 본 발명은 광범위한 항균력을 지닌 신규한 일반식(I)로 표시되는 프로페닐 세펨계 화합물과 그의 약제학적으로 허용되는 염 및 그 제조 방법에 관한 것으로 입체 구조적으로 syn, anti의 두가지 형태의 이성체를 가질 수 있다.
본 발명은 일반식(III)의 3-클로로메틸 세팔로스포린에 트리페닐포스핀과 요오드를 반응시켜 일반식(IV)의 포스포늄일리드를 제조하는 제1공정 ; 일반식(IV)의 포스포늄일리드를 알데히드 화합물과 비티히반응으로 일반식(V)의 3-클로로프로페닐 화합물을 제조하는 제2공정 ; 일반식(V)의 3-클로로프로페닐화합물을 아세톤 존재하에 염화 요오드와 반응시켜 (E)이성체 프로페닐요오드화합물인 일반식(II)의 3-요오드프로페닐 화합물을 제조하는 제3공정과 ; 일반식(II)의 3-요오드프로페닐 화합물과 일반식(VI)의 피리딘-4-티온 유도체를 용매존재하에 짝지음 반응으로 일반식(VII)의 아세테이트 유도체를 제조하는 제4공정 및 일반식(VII)의 아세테이트 유도체에 아니솔과 트리플루오르아세트산을 사용하는 제5공정으로 이루어진 신규한 일반식(I)로 표시되는 프로페닐 세펨계 화합물을 제조하는 것으로, 본 발명의 화합물들은 그람 양성균이나 그람 음성균에 뛰어난 항균력을 나타내므로 세팔로스포린 화합물계열 의약품에 유용하게 사용할 수 있다.
상기 일반식(I)∼(VII)에 있어서, R
1 은 메톡시기, 히드록시기, 2-플루오르에톡시기를 의미하며 R
2 는 메틸기 또는 수소를 의미하고 R
3 는 벤조기나 수소로서 이중고리구조이거나 단환구조를 의미한다.
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