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公开(公告)号：KR101084734B1
公开(公告)日：2011-11-22
申请号：KR1020090010234
申请日：2009-02-09
Applicant: 한국과학기술연구원
IPC: C07D307/90 , C07D307/93
Abstract: 본 발명은 옥사스파이로 화합물 및 이 화합물의 제조방법에 관한 것으로서, 더욱 상세하게는 메틸렌사이클로알칸다이올 유도체와 카르보 화합물을 출발물질로 사용하여 루이스산 존재하에서 프린스 고리화 반응 및 알킬 자리 옮김 반응을 동시에 수행하여 제조된 하기 화학식 1로 표시되는 신규 옥사스파이로 화합물과 이 화합물의 제조방법에 관한 것이다.
상기 화학식 1에서, R
1
및 R
2 는 각각 수소원자; C
1 -C
6 의 알킬기; 또는 할로겐, 니트로, C
1 -C
6 의 알킬, 및 C
1 -C
6 의 알콕시 중에서 선택된 1 내지 3개의 치환체로 치환 또는 비치환된 페닐기를 나타내고, 또한 R
1
및 R
2 는 서로 결합하여 5각형 내지 7각형의 지방족 또는 방향족 고리를 형성할 수 있고, n은 0, 1 또는 2를 나타낸다.
옥사스파이로 화합물, 프린스 반응, 알킬 자리 옮김 반응-
公开(公告)号：KR101035712B1
公开(公告)日：2011-05-19
申请号：KR1020090053364
申请日：2009-06-16
Applicant: 한국과학기술연구원
IPC: C07D493/04 , C07D493/02
Abstract: 본 발명은 1,6-디옥세케인 화합물과 이의 제조방법에 관한 것으로서, 더욱 상세하게는 알렌닐 알코올 또는 알릴 알코올 화합물을 알데하이드 화합물과 루이스산 존재하에서 프린스 고리화 반응을 수행하여 제조된 하기 화학식 1로 표시되는 1,6-디옥세케인 화합물과 이 화합물의 제조방법에 관한 것이다.
상기 화학식 1에서, R은 탄소수 5 내지 15의 아릴기, 또는 질소, 산소 및 황 원자 중에서 선택된 헤테로원자가 1 내지 3개 포함된 탄소수 5 내지 15의 헤테로아릴기를 나타내며; n은 0 또는 1을 나타낸다.
1,6-디옥세케인, 알렌닐 알코올, 알릴 알코올, 루이스산, 프린스반응-
公开(公告)号：KR1020090087732A
公开(公告)日：2009-08-18
申请号：KR1020080013153
申请日：2008-02-13
Applicant: 한국과학기술연구원
IPC: C07D311/26 , C07D311/22 , C07D311/28
Abstract: A method for producing a 1-(2-hydroxyphenyl)buta-2-en-1-one or cromene-4-one derivative is provided to simply synthesize and use as an intermediate of novel medicine. A 1-(2-hydroxyphenyl)buta-2-en-1-one derivative of the chemical formula 1 or cromene-4-one derivative of the chemical formula 2 is produced by reacting derivative of the chemical formula 3 and aldehyde derivative of the chemical formula 4 under the presence of lewis acid catalyst. In the chemical formulas, R1 is hydrogen atom, C1-C10 alkyl group, C5-C15 aryl group or C1-C10 alkyl silyl group, R2 is hydrogen atom, C1-C10 alkyl group or C5-C15 aryl group.
Abstract translation: 提供1-（2-羟基苯基）丁-2-烯-1-酮或色烯-4-酮衍生物的制备方法，简单地合成并用作新药的中间体。 化学式1的1-（2-羟基苯基）丁-2-烯-1-酮衍生物或化学式2的色烯-4-酮衍生物通过使化学式3的衍生物与 化学式4在路易威酸催化剂存在下。 在化学式中，R 1是氢原子，C 1 -C 10烷基，C 5 -C 15芳基或C 1 -C 10烷基甲硅烷基，R 2是氢原子，C 1 -C 10烷基或C 5 -C 15芳基。
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公开(公告)号：KR100478901B1
公开(公告)日：2005-03-28
申请号：KR1020020002789
申请日：2002-01-17
Applicant: 한국과학기술연구원
IPC: C07D307/12
Abstract: 본 발명은 베일리스-힐만 생성물 및 이의 제조방법에 관한 것으로, 구체적으로는 베타위치가 치환된 베일리스-힐만 생성물 및 인듐을 이용하여 통상적인 방법으로는 제조하기 어려운 상기 베일리스-힐만 생성물을 온화한 조건과 용이한 방법으로 제조하는 방법에 관한 것이다.
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公开(公告)号：KR100466371B1
公开(公告)日：2005-01-13
申请号：KR1020030026907
申请日：2003-04-29
Applicant: 한국과학기술연구원
IPC: C12P17/12
Abstract: PURPOSE: Methods for preparing tetrasubstitued pyrazines using baker's yeast are provided, thereby easily and environment-friendly preparing tetrasubstitued pyrazines in water under mild condition. CONSTITUTION: The method for preparing tetrasubstitued pyrazines of formula (2) using baker's yeast comprises the steps of: (1) preparing a solution of baker's yeast; and (2) dissolving beta-keto alpha-oxime carbonyl derivatives of formula (1) in hydrophilic organic solvent and adding the solution into the baker's yeast solution to carry out chemoselective microbial reduction, wherein R1 is methyl, ethyl or phenyl; R2 is hydrogen, methyl or benzyl; R3 is methoxy, ethoxy, benzyloxy or phenylamine; the organic solvent is selected from benzene, toluene and hexane.
Abstract translation: 目的：提供使用面包酵母制备四取代吡嗪的方法，由此在温和条件下容易且环境友好地制备四取代吡嗪在水中。 构成：使用面包酵母制备式（2）的四取代吡嗪的方法包括以下步骤：（1）制备面包酵母溶液; （2）将式（1）的β-酮基α-肟羰基衍生物溶解于亲水性有机溶剂中，并将该溶液加入面包酵母溶液中进行化学选择性微生物还原，其中R1为甲基，乙基或苯基; R2是氢，甲基或苄基; R3是甲氧基，乙氧基，苄氧基或苯胺; 有机溶剂选自苯，甲苯和己烷。
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Patent Agency Ranking
公开(公告)号：KR100437972B1
公开(公告)日：2004-07-02
申请号：KR1020010066578
申请日：2001-10-27
Applicant: 한국과학기술연구원
IPC: C07D413/14
CPC classification number: C07D413/14
Abstract: The present invention relates to substituted pyrrolidinone compounds of formula 1, wherein n is 0 or 1; Aza is a heterocycle optionally substituted with C1-4 alkyl, or C1-4 alkyl substituted with a heterocycle, which represents a saturated or unsaturated five- or six-membered ring having nitrogen(s) as a heteroatom, which are muscarinic acetylcholine receptor agonists and useful as nootropics and therapeutic agents for cerebral neural diseases such as Alzheimer's disease; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.
Abstract translation: 本发明涉及式1的取代的吡咯烷酮化合物，其中n是0或1; Aza是任选被C1-4烷基或被杂环取代的C1-4烷基取代的杂环，所述杂环代表具有氮作为杂原子的饱和或不饱和五元或六元环，其为蕈毒碱乙酰胆碱受体激动剂 作为阿尔茨海默病等脑神经疾病的促智药和治疗药有用; 和其药学上可接受的盐; 其制备方法; 和包含这些化合物或盐的药物组合物。
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公开(公告)号：KR1020030062542A
公开(公告)日：2003-07-28
申请号：KR1020020002789
申请日：2002-01-17
Applicant: 한국과학기술연구원
IPC: C07D307/12
Abstract: PURPOSE: Provided is a method of making β-methyl substituted Baylis-Hillman product represented by the formula(1) with indium easily under mild condition. The product is useful as precursor for the synthesis of carbapenem antibiotics. CONSTITUTION: A method of preparation of making β-methyl substituted Baylis-Hillman product comprises the steps of: making a compound of the formula (IV) by mixing and reacting a compound of the formula (II) with a compound of the formula(III) in a solvent, followed by addition of indium, stirring, reacting with acid and extraction; and adding the compound of the formula(IV) and base. In the formula (IV), R is alkyl, cycloalkyl, aryl or heterocyclic compound; R1 is alkyl, aryl or heterocyclic compound.
Abstract translation: 目的：提供在温和条件下容易地用铟制备由式（1）表示的β-甲基取代的Baylis-Hillman产品的方法。 该产品可用作合成碳青霉烯类抗生素的前体。 构成：制备β-甲基取代的Baylis-Hillman产品的方法包括以下步骤：通过将式（II）化合物与式（III）的化合物混合和反应来制备式（Ⅳ）化合物 ），然后加入铟，搅拌，与酸反应并萃取; 并加入式（IV）和碱的化合物。 在式（Ⅳ）中，R是烷基，环烷基，芳基或杂环化合物; R1是烷基，芳基或杂环化合物。
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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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公开(公告)号：KR1020030034816A
公开(公告)日：2003-05-09
申请号：KR1020010066568
申请日：2001-10-27
Applicant: 한국과학기술연구원
IPC: C07D401/06 , A61K31/435 , A61K31/40
CPC classification number: C07D401/06
Abstract: PURPOSE: A tetrahydropyridine derivative having high affinity for muscarine type acetylcholine receiptor is provided, thereby the tetrahydropyridine derivative can be useful as a recognition improving agent and a nervous disease treating agent. CONSTITUTION: The tetrahydropyridine derivative having high affinity for a muscarine type acetylcholine receiptor is represented by formula(1), wherein m is 0 or 1; n is 1 or 2; R1 is hydrogen, C1-4 alkyl, C2-4 alkynyl or aryl; and R3 is C1-4 alkyl. The process for preparing the tetrahydropyridine derivative comprises (i) condensation of a compound of formula(5) with R1ONH2-HCl to prepare a compound of formula(8); and (ii) reacting the compound of formula(8) with alkyl iodide to prepare alkyl pyrimidine salt and reducing the alkyl pyrimidine salt.
Abstract translation: 目的：提供对毒蕈碱型乙酰胆碱受体具有高亲和力的四氢吡啶衍生物，由此四氢吡啶衍生物可用作识别改善剂和神经疾病处理剂。 构成：对毒蕈碱型乙酰胆碱受体具有高亲和力的四氢吡啶衍生物由式（1）表示，其中m为0或1; n为1或2; R1是氢，C1-4烷基，C2-4炔基或芳基; 并且R 3是C 1-4烷基。 制备四氢吡啶衍生物的方法包括（i）式（5）化合物与R1ONH2-HCl缩合以制备式（8）化合物; 和（ii）使式（8）化合物与烷基碘反应制备烷基嘧啶盐并还原烷基嘧啶盐。
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公开(公告)号：KR100377327B1
公开(公告)日：2003-03-26
申请号：KR1020020036479
申请日：2002-06-27
Applicant: 한국과학기술연구원
IPC: C07D311/16
Abstract: PURPOSE: Provided is a method for preparing allylated 7-hydroxycoumarin derivatives effectively and economically in high yield. CONSTITUTION: The method for preparing allylated 7-hydroxycoumarin is characterized by reacting allylhalide of the formula(1) with 7-hydroxycoumarin of the formula(2) to manufacture allylated 7-hydroxycoumarin derivative of the formula(3).
Abstract translation: 目的：提供一种高产率有效和经济地制备烯丙基化7-羟基香豆素衍生物的方法。 构成：烯丙基化7-羟基香豆素的制备方法的特征在于使式（1）的烯丙基卤化物与式（2）的7-羟基香豆素反应，制备式（3）的烯丙基化7-羟基香豆素衍生物。
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