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公开(公告)号：KR100343947B1
公开(公告)日：2002-07-22
申请号：KR1019990041613
申请日：1999-09-28
Applicant: 한국과학기술연구원
IPC: C07D413/06
Abstract: 본발명은화학식 1을갖는이소옥사졸피페라진계열의화합물또는그 염의제조방법및 상기방법에의해만들어진라이브러리에관한것으로, 상기방법은화학식 2의화합물과화학식 3의화합물을염기및 염소화제의존재하에 1,3-쌍극자고리화첨가반응시켜화학식 1 또는그 염의화합물을제조하는것으로구성된다. 그화학식 1, 2, 3과반응식 1은다음과같다. 상기화학식 1, 2, 3과반응식 1에서, R및 R는페닐, 벤질, 할로겐화페닐, C-C의알킬기로치환된페닐, C-C의알콕시기로치환된페닐, (트리플루오로)메틸페닐, 피리딜등의페닐유도체를말하며, R-R는수소이며, X는질소이며,는이중결합또는삼중결합을의미하며,는이중결합또는단일결합을의미한다.
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2.发明公开도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 失效在DOPAMINE D3和D4受体上具有选择性生物活性的新的4,5-二羟基甲基丙烯酰胺衍生物及其制备方法
公开(公告)号：KR1020020043413A
公开(公告)日：2002-06-10
申请号：KR1020000073122
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08
Abstract: PURPOSE: Provided are novel 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity to dopamine D3 and D4 receptors, and their preparation method by reductive amination in the presence of reductant. CONSTITUTION: 4,5-dihydroisoxazolylalkylpiperazine derivative is represented by the formula(1), wherein R1, R2, R3, R4 and R5 are identical or different from each other, and represents individually hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 alkoxy group, C2-C6 alkenyl group, hydroxy group , hydroxymethyl group, aryl group, heteroaryl group, amino group, C1-C6 alkyl amino group, carbonyl group, C3-C8 cycloalkyl group, or C3-C8 heterocyclic group; R6 represents hydrogen atom, halogen atom, alkyl group, C1-C6 alkoxy group, aryl group, pyridyl group, heterocyclic group or pyrimidyl group; X represents CH or nitrogen atom; and n is 3 or 4.
Abstract translation: 目的：提供对多巴胺D3和D4受体具有选择性生物活性的新型4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下还原胺化的制备方法。 构成：4,5-二氢异恶唑基烷基哌嗪衍生物由式（1）表示，其中R 1，R 2，R 3，R 4和R 5彼此相同或不同，并且表示单独的氢原子，卤素原子，C1-C6烷基， C1-C6烷氧基，C2-C6烯基，羟基，羟甲基，芳基，杂芳基，氨基，C1-C6烷基氨基，羰基，C3-C8环烷基或C3-C8杂环基; R6表示氢原子，卤素原子，烷基，C1-C6烷氧基，芳基，吡啶基，杂环基或嘧啶基; X表示CH或氮原子; n为3或4。
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公开(公告)号：KR1019950006907B1
公开(公告)日：1995-06-26
申请号：KR1019920016613
申请日：1992-09-09
Applicant: 한국과학기술연구원
IPC: C07C405/00
Abstract: The preparation method for 16-phenoxy prostatrienoic acid (I) and its derivatives consists of (1) opening the ring of 1a-hydroxy-4a- (tetrahydropyran- 2-yloxy)-3B-(3a-tetrahydropyran-2-yloxy)-4-phenoxy-19e)buten-1-yl)-cyclopent-2a-yl acetaldehyde lactol (V) with lithium trimethylsilyl acetylide to form 1a-hydroxy-4a- (tetrahydropyran-2-yloxy)-3B-(3a-tetrahydropyran-2-yloxy)-4-phenoxy-19e) but-3-in-2-ol (Ia), (2) rearranging (Ia) with lithium acetylide or ethinyl magnesium halide in tetrahydrofurane to form allen compounds through propargyl ester or ether compounds, to finally obtain (I). (I) is useful for pregnancy control drug when a-hydroxyl group is substituted at carbon position 9, and for control of gastric juice or brochyial expansion when oxygen is at 9.
Abstract translation: 16-苯氧基前列腺三烯酸（I）及其衍生物的制备方法包括：（1）将1a-羟基-4a-（四氢吡喃-2-基氧基）-3B-（3a-四氢吡喃-2-基氧基） 4-苯氧基-19e）丁烯-1-基） - 环戊-2-基乙醛内酯（V）与三甲基甲硅烷基乙炔基锂形成1a-羟基-4a-（四氢吡喃-2-基氧基）-3B-（3a-四氢吡喃-2-基） -2-氧基）-4-苯氧基-19e）丁-3-醇（Ia），（2）用乙炔化锂或乙炔基卤化镁在四氢呋喃中重排（Ia），以通过炔丙基酯或醚化合物形成丙烯化合物 ，终于获得（I）。 （I）在碳位置9替代α-羟基时可用于妊娠控制药物，当氧气为9时用于控制胃液或布朗氏膨胀。
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5.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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Patent Agency Ranking
公开(公告)号：KR1019940007000A
公开(公告)日：1994-04-26
申请号：KR1019920016613
申请日：1992-09-09
Applicant: 한국과학기술연구원
IPC: C07C405/00
Abstract: 본 발명은 16-페녹시 프로스타트리에노산 유도체의 제조에 유용한 중간체(Ⅰ)을 제조하고, 이 화합물을 이용한 다음 일반식(Ⅱ)의 16-페녹시 프로스타트리에노 산 유도체를 제조하는 방법에 관한 것이
상기식에서 R은 테트라하이드로피라닐, 테트라하이드로푸라닐, 2-에톡시에틸 또는 3-t-부틸 디메틸실릴, 트리이소프로필실릴, 트리에틸실릴과 같은 에테르형성그룹으로, R
1 ,R
2 는 수소, 또는 아세틸과 같은 에스테르 형성그룹이고, P는 수소, 트리메틸실릴, 또는 트리부틸틴이고, Z는 산소 또는 α-히드록실기이며, 파상선은 에피입체 혼합물이다.-
公开(公告)号：KR1020010029025A
公开(公告)日：2001-04-06
申请号：KR1019990041613
申请日：1999-09-28
Applicant: 한국과학기술연구원
IPC: C07D413/06
Abstract: PURPOSE: Provided is a method for manufacturing an iso-oxazole piperazin compound and its salts which can end up developing a lead compound for new drugs. CONSTITUTION: An isooxazol compound is manufactured by the next step: reacting the compound of the formula (2) with the compound of the formula (3) at room temperature, at 0-7 deg.C, in the presence of organic solvent, 0.1-2 equivalent, preferably 1 equivalent of base, and chlorinating agent for 30 minutes-4 hours, preferably 2 hours. Wherein, organic solvent is selected from benzene, methylene chloride, and tetrahydrofuran; a base is selected from methyl amine, ethyl amine, diethyl amine, dimethyl amine, trimethyl amine, cyclohexylamine, diethylisopropylamine, pyridine, or preferably triethylamine; And chlorinating agent is one of chlorine, N-chlorosuccinimide, and sodium hypochlorite. In the formula (1), (2), and (3), R1 and R6 are a phenyl group, benzyl group, halide phenyl group, phenyl group having substituted C1-C6 alkyl group, phenyl group having substituted C1-C6 alkoxy group, methyl phenyl group, or pyridyl group. R2-R5 is hydrogen, and X is nitrogen.
Abstract translation: 目的：提供一种制造异恶唑哌嗪化合物及其盐的方法，其可以最终形成用于新药的铅化合物。 构成：通过下一步骤制备异恶唑化合物：在室温，0-7℃，有机溶剂存在下，将式（2）化合物与式（3）化合物反应，得到0.1 -2当量，优选1当量碱和氯化剂30分钟-4小时，优选2小时。 其中有机溶剂选自苯，二氯甲烷和四氢呋喃; 碱选自甲胺，乙胺，二乙胺，二甲胺，三甲胺，环己胺，二乙基异丙胺，吡啶，或优选三乙胺; 而氯化剂是氯，N-氯代琥珀酰亚胺和次氯酸钠之一。 在式（1），（2）和（3）中，R 1和R 6是苯基，苄基，卤化苯基，具有取代的C 1 -C 6烷基的苯基，具有取代的C 1 -C 6烷氧基的苯基 ，甲基苯基或吡啶基。 R2-R5是氢，X是氮。
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公开(公告)号：KR1019940007042A
公开(公告)日：1994-04-26
申请号：KR1019920017443
申请日：1992-09-24
Applicant: 한국과학기술연구원
IPC: C07D501/46
Abstract: 본 발명은 항생제로 표시되는 신규
본 발명은 광범위한 항균력을 나타내는, 항생제로서 유용한 다음 일반식(Ⅰ)의 세팔로스포린 화합물 및 그 제조방법에 관한 것이다.
R
1 은 메틸 혹은 1-카르복시-1-메틸에틸기이고, R
2 는 메틸 또는 아미노기이며, R
3 는 2-히드록시에틸, 2,3-디히드록시프로필, 시클로프로필, 페닐, 3,4-메틸렌디옥시페닐, 6-클로로-3,4-메틸렌디옥시페닐, 3-시아노-2-피리딜, 3-히드록시-2-피리딜, 2-피라질, 2-티아졸릴, 2-(2-아미노티아졸-4-일)-2-(Z)-메톡시이미노아세틸, 2-티오펜카르보닐, 3-티오펜카르보닐, 시클로프로판카르보닐, 메톡시카르보닐, 메틸티오카바모일, 아미노, 아세트아미도, 페닐아세트아미도, 2-티오펜아세트아미도, 2-(2-아미노티아졸-4-일)-2-(Z)-메톡시이미노아세트아미도, 니트로소아미노, 니트로소, 2,4,6-트리메틸벤젠술포닐, 4-클로로벤젠술포닐, 트리플루오로메탄술포닐, 3,4-디히드록시벤즈이미노이다. -
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