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公开(公告)号：KR1019920008164B1
公开(公告)日：1992-09-24
申请号：KR1019900011884
申请日：1990-08-02
Applicant: 한국화학연구원
IPC: C07D401/04
Abstract: Quinoline derivs. of formula (I) and their pharmaceutically acceptable salts are prepd. by condensing a tetrahydropyridine deriv. of formula (II) and a quinoline carboxylic acid deriv. of formula (III) at 200 deg.C for 1-10 hr(s) in the presence (or absence) of a solvent, and in the presence of a base. In the formulas, R1= ethyl, cyclopropyl or 2,4-difluorophenyl; R2 and R3=H, F or amino; R4 and R5=H, C1-3 alkyl, C1-3 alkyl substd. N- alkylhydroxyamino or N-alkoxy- N-alkylamino; R6=H or C1-3 lower alkyl; X=N, methyne, fluoromethyne or ethyne. Cpds. (I) are useful as an antibacterial agent.
Abstract translation: 喹啉衍生物。 的式（I）化合物及其药学上可接受的盐是制备的。 通过缩合四氢吡啶衍生物。 的式（II）和喹啉羧酸衍生物。 在存在（或不存在）溶剂的情况下，在存在碱的情况下，在200℃下进行1-10小时。 式中R 1 =乙基，环丙基或2,4-二氟苯基; R2和R3 = H，F或氨基; R4和R5 = H，C1-3烷基，C1-3烷基。 N-烷基羟基氨基或N-烷氧基-N-烷基氨基; R6 = H或C1-3低级烷基; X = N，甲炔，氟甲炔或乙炔。 CPDS。 （I）可用作抗菌剂。
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公开(公告)号：KR1019920005745B1
公开(公告)日：1992-07-18
申请号：KR1019900004181
申请日：1990-03-28
Applicant: 한국화학연구원
IPC: C07D498/04 , C07D498/06
Abstract: Benzoxazine derivs. of formula (I) and their pharmaceutically acceptable acid addn. salts are new. In (I), R1 and R2 each = H or lower alkyl; n = 1 or 2. Also clainned is the prepn. of (I) which comprises reacting a benzoxazine carboxylic acid deriv. of formula (II) with a cpd. of formula (III) at room temp. -200 deg.C for 1- 10 hr(s). In (II), X= halogen. The cpds. (I) have a good antibacterial activity, a broad spectrum activity, low toxicity and high bioavailability.
Abstract translation: 苯并恶嗪衍生物。 的式（I）化合物及其药学上可接受的酸加成。 盐是新的。 在（I）中，R 1和R 2各自为H或低级烷基; n = 1或2.也是准备工作。 的（I），其包括使苯并恶嗪羧酸衍生物反应。 的式（II）与cpd。 的式（III）。 -200℃，持续1-10小时（s）。 在（II）中，X =卤素。 cpds。 （I）具有良好的抗菌活性，广谱活性，低毒性和高生物利用度。
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公开(公告)号：KR1019920006315A
公开(公告)日：1992-04-27
申请号：KR1019900015166
申请日：1990-09-25
Applicant: 한국화학연구원
IPC: C07D211/70
Abstract: 내용 없음
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Patent Agency Ranking
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37.发明授权광학 활성을 갖는 (4Ｒ, 6Ｒ)-6-(2-아미노에틸)-4-하이드록시-테트라하이드로피란-2-온 유도체의 제조방법 有权制备光学纯（4R，6R）-6-（2-氨基乙基）-4-羟基 - 四氢吡喃-2-酮衍生物的方法
公开(公告)号：KR101069698B1
公开(公告)日：2011-10-04
申请号：KR1020080084248
申请日：2008-08-28
Applicant: 한국화학연구원
Inventor： 김문환
IPC: C07D309/16
Abstract: 본발명은광학활성을갖는 (4R, 6R)-6-(2-아미노에틸)-4-하이드록시-테트라히드로피란-2-온유도체의제조방법에관한것으로서, 본발명의제조방법에따르면고지혈증치료제인아토르바스타틴을제조하기위한핵심중간체로서유용한광학활성을갖는 (4R, 6R)-6-(2-아미노에틸)-4-하이드록시-테트라하이드로피란-2-온유도체를온화한조건하에서간편하게고수율및 저비용으로합성할수 있다.
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公开(公告)号：KR1020100026239A
公开(公告)日：2010-03-10
申请号：KR1020080085164
申请日：2008-08-29
Applicant: 한국화학연구원
IPC: C07D311/92 , C09K9/02
Abstract: PURPOSE: A novel method for economically manufacturing naphthopyran based photochromic dye of high yield and high purity is provided. CONSTITUTION: A method for manufacturing naphthopyran based photochromic dye of chemical formula 1 comprises: a step of reacting amino naphtholic acid with alkyl- or benzyl-chloroformate to obtain a compound of chemical formula 4; a step of substituting the compound of chemical formula 4 with amine compound to obtain a compound of chemical formula 2; a step of reacting halogen-substituted benzo phenone with nucleophilic compound under the presence of base and reacting with sodium acetylide to obtain a compound of chemical formula 3; and a step of reacting the compound of chemical formula 3 with a compound of chemical formula 2.
Abstract translation: 目的：提供一种经济地制备高产率，高纯度的萘并吡喃基光致变色染料的新方法。 构成：制备化学式1的萘并吡喃基光致变色染料的方法包括：使氨基萘酚与烷基或苄基氯甲酸酯反应得到化学式4化合物的步骤; 用胺化合物代替化学式4的化合物以获得化学式2的化合物的步骤; 在碱存在下使卤素取代的苯并苯酮与亲核化合物反应并与乙炔化钠反应以获得化学式3化合物的步骤; 和使化学式3的化合物与化学式2的化合物反应的步骤。
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公开(公告)号：KR100532042B1
公开(公告)日：2005-11-30
申请号：KR1020030051360
申请日：2003-07-25
Applicant: 한국화학연구원 , 한국유나이티드제약 주식회사
IPC: C07C213/08
Abstract: 본 발명은 고지혈증 치료제인 아토르바스타틴을 제조하기 위한 핵심 중간체인, 질소가 이중치환된 7-아미노-3,5-디하이드록시 헵탄산 유도체의 제조방법에 관한 것으로, 질소를 이중 보호시킨 케토에스테르를 고압 수소화 반응시키는 것을 포함하는 본 발명의 방법에 의하면, 화학식 2로 표시되는 질소가 이중치환된 7-아미노-3,5-디하이드록시 헵탄산 유도체를 종래의 방법에 비해 온화한 조건하에서 간편하게 고수율로 합성할 수 있다.
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40.发明公开질소가 이중치환된 7-아미노-3,5-디하이드록시 헵탄산유도체의 제조방법 有权具有脱氨基氮的7-氨基-3,5-二羟基乙酸衍生物的制备，其为制备ATORVASTATIN的中间体作为超临界药物治疗
公开(公告)号：KR1020050012408A
公开(公告)日：2005-02-02
申请号：KR1020030051360
申请日：2003-07-25
Applicant: 한국화학연구원 , 한국유나이티드제약 주식회사
IPC: C07C213/08
Abstract: PURPOSE: Provided is a method of preparing 7-amino-3,5-dihydroxyheptanoic acid derivatives with disubstituted nitrogen, an intermediate for producing atorvastatin (Liptor) as a medical treatment for hyperlipemia, which is inhibitor of HMG-CoA reductase and ACAT. CONSTITUTION: The preparation method comprises: (A) performing high pressure hydrogenation of the compound of formula 3 in the presence of Ru catalyst at room temperature-100deg.C under 30-100atm to produce the compound of formula 4; (B) reacting compound of formula 4 with the compound of formula 5 to produce the compound of formula 6; and (C) carrying out high pressure hydrogenation of compound of formula 6 in the presence of Ru catalyst at room temperature-100deg.C under 30-100atm or stereoselective hydrogenation using diethylmethoxy borane or sodium borohydride. In the formula, R is C1-6 alkyl; P and P1 are independently benzyl, benzyloxycarbonyl, C1-6 alkyloxycarbonyl, benzoyl or acetyl.
Abstract translation: 目的：提供一种制备具有二取代氮的7-氨基-3,5-二羟基庚酸衍生物的方法，其为生产阿托伐他汀（Liptor）作为HMF-CoA还原酶和ACAT抑制剂的高脂血症药物治疗中间体。 制备方法：（A）在室温-10℃下，在30-100atm下，在Ru催化剂存在下，对式3化合物进行高压氢化，得到式4化合物; （B）使式4的化合物与式5的化合物反应以制备式6的化合物; 和（C）使用二乙基甲氧基硼烷或硼氢化钠，在室温-10℃下，在30-100atm或立体选择性氢化下，在Ru催化剂存在下，使式6化合物进行高压氢化。 在该式中，R为C 1-6烷基; P和P1独立地是苄基，苄氧基羰基，C 1-6烷氧基羰基，苯甲酰基或乙酰基。
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