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公开(公告)号：KR1020090090457A
公开(公告)日：2009-08-26
申请号：KR1020080015671
申请日：2008-02-21
Applicant: 한국화학연구원
IPC: C07D401/08 , A61K31/497
Abstract: A piperazine derivative is provided to treat schizophrenia by antagonism to dopamine D4 receptor. A piperazine derivative is denoted by the chemical formula 1. In the chemical formula 1, R1 is structural formula a, b, c, d, e, or f, and X is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy or cyano. A method for producing the piperazine derivative of the chemical formulal Ia: a step of reacting hydrazine in substituted acetone phenone to generate hydrazone and reacting ammonium acetate to produce pyrrole ring of the chemical formula III; a step of reacting with cycloalkane under the presence of catalyst to produce a cycloalkine pyrrole; and a step of reacting reductive amination with substituted or non-substituted piperazine to produce a compound of the chemical formula Ia.
Abstract translation: 提供哌嗪衍生物通过拮抗多巴胺D4受体来治疗精神分裂症。 哌嗪衍生物由化学式1表示。在化学式1中，R 1为结构式a，b，c，d，e或f，X为氢，卤素，C 1-6烷基，C 1-6烷氧基 或氰基。 制备化学式Ia的哌嗪衍生物的方法：使肼在取代的丙酮苯酮中反应生成腙并使乙酸铵反应生成化学式III的吡咯环的步骤; 在催化剂存在下与环烷烃反应生成环烷基吡咯的步骤; 以及使还原胺化与取代或未取代的哌嗪反应以产生化学式Ia的化合物的步骤。
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42.发明授权베타-세크리테아제의 활성을 저해하는 아릴피페라진이 치환된 피페리딘 유도체 또는 이의 약제학적으로 허용 가능한 염 및 이를 유효성분으로 함유하는 신경퇴행성 질환의 예방 또는 치료용 조성물 失效抑制β-分泌酶活性的4-芳基哌嗪-1-基哌啶衍生物或含有该β-分泌酶活性的药物组合物和用于预防和治疗含有其作为活性成分的神经变性疾病的组合物
公开(公告)号：KR100894713B1
公开(公告)日：2009-04-24
申请号：KR1020070101067
申请日：2007-10-08
Applicant: 한국화학연구원
IPC: C07D401/04 , A61K31/497 , A61P25/28
Abstract: 본 발명은 베타-세크리테아제의 활성을 저해하는 아릴피페라진이 치환된 피페리딘 화합물 또는 이의 약제학적으로 허용 가능한 염 및 이를 유효성분으로 함유하는 신경퇴행성 질환의 예방 또는 치료용 조성물에 관한 것으로, 본 발명에 따른 아릴 피페라진이 치환된 피페리딘 유도체는 베타-세크리테아제 저해 활성이 우수하므로, 알츠하이머, 다운증후군 등의 신경퇴행성 질환의 예방 및 치료에 유용하게 사용될 수 있다.
알츠하이머 질환, 피페리딘 화합물, 베타-세크리테아제, 노화, 신경퇴행성 질환, 베타-아밀로이드-
公开(公告)号：KR100786371B1
公开(公告)日：2007-12-17
申请号：KR1020060123826
申请日：2006-12-07
Applicant: 한국화학연구원
IPC: C07D491/04
Abstract: A method for preparing galantamine is provided to synthesize the highly pure galantamine, known to show the excellent dementia treating effect, with high yield. A method for preparing galantamine comprises the steps of: (a) after reacting an oxazolidinone derivative represented by the formula(2) with an aromatic halide derivative represented by the formula(3), removing a hydroxy protection group from the product to prepare a phenol derivative represented by the formula(4b)(wherein X is a halogen atom, and Pro is a hydroxy protection group); (b) subjecting the compound of the formula(4b) in the presence of an oxidizer to an oxidative coupling reaction to prepare a spiro benzo azepine derivative represented by the formula(5); (c) reacting the compound of the formula(5) with morpholine using a Pd catalyst to prepare a stereoselective hydrofuran derivative represented by the formula(6); (d) converting C-6 hydroxy group of the compound of the formula(6) into a hydrogen atom to prepare a compound represented by the formula(7b); (e) reducing C-10 ketone of the compound of the formula(7b) to prepare a compound represented by the formula(8); (f) after hydrolyzing the compound of the formula(8) under the base condition to open an oxazolidinone ring, subjecting the product to an N-methylation reaction to prepare a compound represented by the formula(9b); (g) oxidizing the compound of the formula(9b) to prepare a compound represented by the formula(10); (h) after converting an aldehyde group of the compound of the formula(1) into oxime, dehydrating the product to prepare a compound represented by the formula(11); and (i) reducing C-6 ketone of the compound of the formula(11) and eliminating C-10 carbonitrile of the compound to prepare the galantamine represented by the formula(1).
Abstract translation: 提供一种制备加兰他敏的方法，以合成具有优异痴呆治疗效果的高纯度加兰他敏，产率高。 制备加兰他敏的方法包括以下步骤：（a）使由式（2）表示的恶唑烷酮衍生物与由式（3）表示的芳族卤化物衍生物反应后，从产物中除去羟基保护基以制备苯酚 衍生物（4b）（其中X是卤素原子，Pro是羟基保护基团）; （b）在氧化剂存在下将式（4b）化合物进行氧化偶联反应，制备由式（5）表示的螺苯并吖庚因衍生物; （c）使用Pd催化剂使式（5）的化合物与吗啉反应，制备由式（6）表示的立体选择性氢呋喃衍生物; （d）将式（6）化合物的C-6羟基转化为氢原子，制备式（7b）表示的化合物。 （e）还原式（7b）化合物的C-10酮以制备由式（8）表示的化合物; （f）在碱性条件下水解式（8）化合物以打开恶唑烷酮环后，使产物进行N-甲基化反应以制备式（9b）表示的化合物; （g）氧化式（9b）化合物以制备由式（10）表示的化合物; （h）将式（1）化合物的醛基转化为肟后，使产物脱水，制备式（11）表示的化合物; 和（i）还原式（11）化合物的C-6酮并除去该化合物的C-10腈，以制备由式（1）表示的加兰他敏。
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44.发明公开무스카린 수용체 작용물질로서 작용하는1,2,3,4-테트라하이드로피리미디닐-1,2,4-옥사다이아졸유도체와 이의 제조방법 失效1,2,3,4-四氢吡啶并咪唑-1,2,4-氧杂吖啶衍生物作为抑制剂受体激动剂及其制备方法
公开(公告)号：KR1020060032771A
公开(公告)日：2006-04-18
申请号：KR1020040081725
申请日：2004-10-13
Applicant: 한국화학연구원
IPC: C07D413/04
Abstract: 본 발명은 무스카린 수용체 작용물질로서 작용하는 신규 1,2,3,4-테트라하이드로피리미디닐-1,2,4-옥사다이아졸 유도체와 이의 제조방법, 그리고 상기 신규 화합물을 유효성분으로 함유하는 약제조성물에 관한 것이다.
본 발명에 따른 1,2,3,4-테트라하이드로피리미디닐-1,2,4-옥사다이아졸 유도체는 무스카린 수용체 작용물질(muscarinic receptor agonist)로서 활성을 나타내므로 기억항진 및 노인성 치매 치료제, 뇌질환 및 중추신경계에 관련된 치료약물에 응용될 수 있고, 테트라하이드로피리딘의 등배전자(bioisoster)로 작용하여 이미 임상적으로 치매 치료제에 사용되는 아레콜린 및 밀라멜린 약제와 대등한 치료효과를 나타낸다.
노인성 치매 치료제, 무스카린 수용체 작용물질, 1,2,3,4-테트라하이드로피리미디닐-1,2,4-옥사다이아졸 유도체-
公开(公告)号：KR100402054B1
公开(公告)日：2003-10-17
申请号：KR1020010016968
申请日：2001-03-30
Applicant: 한국화학연구원
IPC: C07D405/14
Abstract: PURPOSE: Provided is 2-aryl-2-methyl-2,3-dihydrobenzofuran with antioxidant activity which is useful for the prevention and treatment of various diseases associated with active oxygen species. CONSTITUTION: The 2-aryl-2-methyl-2,3-dihydrobenzofuran with antioxidant activity represented by formula(1) and its pharmaceutically acceptable salts are provided, wherein R' is hydrogen, acetyl, or t-butyldimethylsilyl; R is NO2, NH2, COOR1, CONR2R3 or NHC(Z)R4; R1 is hydrogen, C1 to C8 alkyl, C3 to C10 alkenyl, C3 to C6 cycloalkyl, phenyl or pyrimidine; R2 and R3 are independently C1 to C8 alkyl, phenyl, or pyridine; R4 is C1 to C8 alkyl, C3 to C10 alkenyl, phenyl, pyridine, C1 to C6 alkylamine, aniline, or aminopyridine; and Z is oxygen or sulfur. Its preparing method comprises the steps of: alkylation of a compound of formula(2) with a compound of formula(3) to form a compound of formula(4); Claisen reaction of the compound of formula(4) to form a compound of formula(5); and cyclization of the compound of formula(5) to prepare a compound of formula(1).
Abstract translation: 目的：提供具有抗氧化活性的2-芳基-2-甲基-2,3-二氢苯并呋喃，其用于预防和治疗与活性氧物质有关的各种疾病。 构成：提供式（1）代表的具有抗氧化活性的2-芳基-2-甲基-2,3-二氢苯并呋喃及其药学上可接受的盐，其中R'为氢，乙酰基或叔丁基二甲基甲硅烷基; R为NO2，NH2，COOR1，CONR2R3或NHC（Z）R4; R1为氢，C1至C8烷基，C3至C10烯基，C3至C6环烷基，苯基或嘧啶; R2和R3独立地为C1至C8烷基，苯基或吡啶; R4为C1至C8烷基，C3至C10链烯基，苯基，吡啶，C1至C6烷基胺，苯胺或氨基吡啶; Z是氧或硫。 其制备方法包括以下步骤：用式（3）化合物将式（2）化合物烷基化以形成式（4）化合物; 式（4）化合物克莱森反应形成式（5）化合物; 和式（5）化合物环化制备式（1）化合物。
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Patent Agency Ranking
公开(公告)号：KR100392074B1
公开(公告)日：2003-08-19
申请号：KR1020000056263
申请日：2000-09-25
Applicant: 한국화학연구원
IPC: A01N43/78
Abstract: PURPOSE: A new thiazole derivative obtained by using amide as a starting material is provided which has a strong antibacterial effect on plant pathogenic bacteria with a small amount, for example Pyricularia oryzae Cavera, Rhizoctonia SolaniAG-1, Botrytis cinerea KCI, Phytophthora infestans or the like. CONSTITUTION: Thioamide(formula II) is dissolved in dichloroethane, agitated with dichloroacetone at room temperature for 48 to 72 hr in the presence of a base and then dehydrated to produce chloromethyl thiazole(formula III). A chlorine atom of the chloromethyl thiazole is substituted to an iodine atom by use of sodium iodide and then reacted with 2-(2-hydroxyphenyl)-3-methoxy acrylic acid methylester(formula IV)(in case of A=C) or 2-methoxyimino-(2-hydroxyphenyl)-acetic acid methylester(formula IV)(in case of A=N) to produce a thiazole derivative(formula I).
Abstract translation: 目的：提供一种以酰胺为起始原料得到的新型噻唑衍生物，对植物病原菌有较强的抗菌作用，如Pyricularia oryzae Cavera，Rhizoctonia SolaniAG-1，Botrytis cinerea KCI，致病疫霉或 喜欢。 构成：将硫代酰胺（式II）溶于二氯乙烷中，在室温下用二氯丙酮搅拌48-72小时，然后脱水，生成氯甲基噻唑（式III）。 通过使用碘化钠将氯甲基噻唑的氯原子取代为碘原子，然后与2-（2-羟基苯基）-3-甲氧基丙烯酸甲酯（式IV）（在A = C的情况下）或2 （2-羟基苯基） - 乙酸甲酯（式IV）（在A = N的情况下）反应以产生噻唑衍生物（式I）。
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公开(公告)号：KR1020020076826A
公开(公告)日：2002-10-11
申请号：KR1020010016968
申请日：2001-03-30
Applicant: 한국화학연구원
IPC: C07D405/14
Abstract: PURPOSE: Provided is 2-aryl-2-methyl-2,3-dihydrobenzofuran with antioxidant activity which is useful for the prevention and treatment of various diseases associated with active oxygen species. CONSTITUTION: The 2-aryl-2-methyl-2,3-dihydrobenzofuran with antioxidant activity represented by formula(1) and its pharmaceutically acceptable salts are provided, wherein R' is hydrogen, acetyl, or t-butyldimethylsilyl; R is NO2, NH2, COOR1, CONR2R3 or NHC(Z)R4; R1 is hydrogen, C1 to C8 alkyl, C3 to C10 alkenyl, C3 to C6 cycloalkyl, phenyl or pyrimidine; R2 and R3 are independently C1 to C8 alkyl, phenyl, or pyridine; R4 is C1 to C8 alkyl, C3 to C10 alkenyl, phenyl, pyridine, C1 to C6 alkylamine, aniline, or aminopyridine; and Z is oxygen or sulfur. Its preparing method comprises the steps of: alkylation of a compound of formula(2) with a compound of formula(3) to form a compound of formula(4); Claisen reaction of the compound of formula(4) to form a compound of formula(5); and cyclization of the compound of formula(5) to prepare a compound of formula(1).
Abstract translation: 目的：提供具有抗氧化活性的2-芳基-2-甲基-2,3-二氢苯并呋喃，其可用于预防和治疗与活性氧相关的各种疾病。 构成：提供了具有由式（1）表示的抗氧化活性的2-芳基-2-甲基-2,3-二氢苯并呋喃及其药学上可接受的盐，其中R'是氢，乙酰基或叔丁基二甲基甲硅烷基; R为NO2，NH2，COOR1，CONR2R3或NHC（Z）R4; R1是氢，C1至C8烷基，C3至C10烯基，C3至C6环烷基，苯基或嘧啶; R2和R3独立地为C1至C8烷基，苯基或吡啶; R4是C1至C8烷基，C3至C10烯基，苯基，吡啶，C1至C6烷基胺，苯胺或氨基吡啶; Z是氧或硫。 其制备方法包括以下步骤：用式（3）化合物烷基化式（2）化合物以形成式（4）化合物; 式（4）化合物的Claisen反应形成式（5）化合物; 和式（5）化合物环化以制备式（1）化合物。
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