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11.发明公开신규 티에노피리미딘 유도체, 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 약학적 조성물 有权新型三硝基嘧啶衍生物，其药物可接受的盐，其制备方法和药物组合物，用于预防或治疗含有其作为活性成分的增殖性疾病
公开(公告)号：KR1020120053648A
公开(公告)日：2012-05-29
申请号：KR1020100114874
申请日：2010-11-18
Applicant: 한국화학연구원
IPC: C07D495/04 , A61K31/519 , A61P35/00
Abstract: PURPOSE: A pharmaceutical composition containing thienopyrimidine derivative is provided to prevent or treating abnormal cell growth diseases. CONSTITUTION: A thienopyrimidine derivative is denoted by chemical formula 1. A method for preparing the derivative comprises: a step of reacting a compound of chemical formula 2 with formamide to prepare a compound of chemical formula 3; a step of substituting the compound of chemical formula 3 to prepare a compound of chemical formula 4; a step of coupling the compound of chemical formula 4 with a compound of chemical formula 5 to prepare a compound of chemical formula 1a. A pharmaceutical composition for preventing or treating abnormal cell growth diseases contains the derivative or pharmaceutically acceptable salt thereof as an active ingredient.
Abstract translation: 目的：提供含有噻吩并嘧啶衍生物的药物组合物，用于预防或治疗异常细胞生长疾病。 构成：噻吩并嘧啶衍生物由化学式1表示。制备衍生物的方法包括：使化学式2的化合物与甲酰胺反应以制备化学式3的化合物的步骤; 用化学式3的化合物代替化学式4的化合物的步骤; 将化学式4的化合物与化学式5的化合物偶联以制备化学式1a的化合物的步骤。 用于预防或治疗异常细胞生长疾病的药物组合物含有其衍生物或药学上可接受的盐作为活性成分。
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公开(公告)号：KR1020100038052A
公开(公告)日：2010-04-12
申请号：KR1020090090692
申请日：2009-09-24
IPC: C07D239/54 , A01N43/54 , A01N41/06
CPC classification number: C07D239/54 , A01N43/54
Abstract: PURPOSE: A herbicide containing uracil compound as an active ingredient is provided to use as a non-selective herbicide which removes broad weeds. CONSTITUTION: A uracil compound is denoted by chemical formula 1. A herbicide contains the uracil compound of chemical formula 1, agriculturally acceptable salt or mixture thereof as an active ingredient. A herbicide composition contains 0.1-99.9 weight% of uracil compound of chemical formula 1, its agriculturally acceptable salt, or mixture thereof, and 0.1-99.9 weight% of additive of surfactant, or solid or liquid diluents. The composition is formulated in a form of suspension, emulsion, liquid, dispersion liquid, or tablet.
Abstract translation: 目的：提供含有尿嘧啶化合物作为活性成分的除草剂，用作去除宽阔杂草的非选择性除草剂。 构成：尿嘧啶化合物由化学式1表示。除草剂含有化学式1的尿嘧啶化合物，农业上可接受的盐或其混合物作为活性成分。 除草剂组合物含有0.1-99.9重量％的化学式1的尿嘧啶化合物，其农业上可接受的盐或其混合物，和0.1-99.9重量％的表面活性剂添加剂，或固体或液体稀释剂。 将组合物配制成悬浮液，乳液，液体，分散液或片剂的形式。
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13.发明公开신규 벤즈옥사졸로 치환된 피리딘 유도체 또는 이의약학적으로 허용가능한 염, 이의 제조방법 및 이를유효성분으로 함유하는 이상세포 성장 질환의 예방 및치료용 약학적 조성물 失效新颖的苯并噻唑衍生物或其药物可接受的盐，其制备方法和药物组合物，用于预防和治疗含有作为活性成分的异常细胞生长疾病
公开(公告)号：KR1020090118601A
公开(公告)日：2009-11-18
申请号：KR1020080044485
申请日：2008-05-14
Applicant: 한국화학연구원
IPC: C07D413/04 , C07D413/02 , A61P35/00
CPC classification number: C07D413/14
Abstract: PURPOSE: A pharmaceutical composition containing pyridine derivative which is substituted with a novel benzoxazole is provided to ensure high effect to protein kinase in treating cell proliferation disorder. CONSTITUTION: A pyridine derivative which is substituted with a benzoxazole is denoted by the chemical formula 1. A method for preparing the derivative or its pharmaceutically acceptable salt comprises: a step of reacting a compound of the chemical formula 2 with a compound of the chemical formula 3 under the presence of metal; and a step of performing deprotection of a compound of the chemical formula 4.
Abstract translation: 目的：提供一种含有新的苯并恶唑代替的吡啶衍生物的药物组合物，以确保蛋白激酶在治疗细胞增殖紊乱中的高效应。 构成：用苯并恶唑取代的吡啶衍生物由化学式1表示。制备衍生物或其药学上可接受的盐的方法包括：使化学式2化合物与化学式 3在金属的存在下; 以及对化学式4的化合物进行脱保护的工序。
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公开(公告)号：KR100552133B1
公开(公告)日：2006-02-14
申请号：KR1020030028254
申请日：2003-05-02
Applicant: 한국화학연구원
IPC: C07D263/58
CPC classification number: C07D213/643 , C07B2200/07 , C07C67/31 , C07C253/30 , C07D241/44 , C07D263/58 , C07C69/712 , C07C255/55
Abstract: 본 발명은 광학활성 (Ｒ)-아릴옥시 프로피온산 에스터 유도체의 제조방법에 관한 것으로서, 보다 상세하게는 여러 관능기로 치환된 페놀 유도체와 (S)-알킬 O-아릴설포닐 락테이트를 반응물질로 사용하여 특정의 용매와 염기 및 온도조건에서 친핵치환 반응시켜 우수한 광학순도 및 생성수율로 다음 화학식 1로 표시되는 (Ｒ)-아릴옥시 프로피온산 에스터 유도체를 경제적으로 제조하는 방법에 관한 것이다.
[화학식 1]
상기 화학식 1에서, R
1 및 A는 각각 발명의 상세한 설명에서 정의한 바와 같다.
(S)-알킬 O-아릴설포닐 락테이트, (S)-에틸 Op-톨루엔설포닐 락테이트, (6-클로로-2-벤족사졸릴옥시)페닐, (6-클로로-2-벤즈티아졸릴옥시)페닐, (6-클로로퀴녹사졸릴옥시)페닐, 비극성 용매, 자일렌, 사이클로헥산, (R)-에틸 2-[4-(6-클로로벤족사졸릴옥시)펜옥시]프로피오네이트, 광학 활성-
公开(公告)号：KR100545784B1
公开(公告)日：2006-01-24
申请号：KR1020030069321
申请日：2003-10-06
Applicant: 한국화학연구원
IPC: C07D401/12
Abstract: 본 발명은 과수원 등의 비선택성 제초제로서 뿐만 아니라 옥수수, 콩과 같은 유용한 작물에는 약해를 주지 않으면서 소량의 처리로 화본과 및 광엽잡초를 선택적으로 방제할 수 있는 다음 화학식 1로 표시되는 신규 구조의 3,4,5,6-테트라히드로프탈이미드계 화합물과 이 화합물을 유효성분으로 함유하는 제초제에 관한 것이다.
상기 화학식 1에서, n, X 및 R은 각각 발명의 상세한 설명에서 정의된 바와 같다.
3,4,5,6-테트라히드로프탈이미드, 제초제, 화본과, 광엽잡초, 선택성Abstract translation: （1）能够选择性地控制与处理的少量hwabongwa和阔叶杂草由下式表示的新颖的结构的本发明3以及非选择性除草剂如果园而不导致植物毒性，有用作物如玉米，豆类 ，基于4,5,6-四氢邻苯二甲酰亚胺的化合物和含有这些化合物作为活性成分的除草剂。
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Patent Agency Ranking
公开(公告)号：KR1020020083568A
公开(公告)日：2002-11-04
申请号：KR1020010022944
申请日：2001-04-27
Applicant: 한국화학연구원
IPC: C07C317/32
Abstract: PURPOSE: Provided is a method for economically synthesizing glibenclamide, with powder shape, which is used as an intermediate for synthesis of medicine useful for treatment of diabetes. CONSTITUTION: The method comprises the steps of (i) reacting N-phenethyl-5-chloro-2-methoxybenzamide with chlorosulfonic acid(ClSO3H) represented by formula 2 in the presence of thionyl chloride(SOCl2) to form p-(N-phenethyl-5-chloro-2-methoxybenzamide)sulfonylchloride represented by formula 3; (ii) reacting sulfonylchloride compound represented by formula 3 with ammonia to form p-(N-phenethyl-5-chloro-2-methoxybenzamide)sulfoneamide represented by formula 4; (iii) reacting sulfoneamide compound represented by formula with alkali metal hydroxide in the presence of alcohol solvent to form p-(N-phenethyl-5-chloro-2-methoxybenzamide)sulfone amide-metal salt represented by formula 5; and (iv) reacting the metal represented by formula 5 with cyclohexyl isocyanate or phenylcyclohexyl carbamate to form glibenclamide represented by formula 1.
Abstract translation: 目的：提供一种经济合成格列本脲的方法，其具有粉末形状，用作合成用于治疗糖尿病的药物的中间体。 方法：该方法包括以下步骤：（i）使N-苯乙基-5-氯-2-甲氧基苯甲酰胺与亚硫酰氯（SOCl 2）存在下由式2表示的氯磺酸（ClSO 3 H）反应，形成对 - （N-苯乙基 -5-氯-2-甲氧基苯甲酰胺）磺酰氯; （ii）使由式3表示的磺酰氯化合物与氨反应以形成由式4表示的对 - （N-苯乙基-5-氯-2-甲氧基苯甲酰胺）磺酰胺; （iii）在醇溶剂存在下使由式表示的磺酰胺化合物与碱金属氢氧化物反应，形成由式5表示的对 - （N-苯乙基-5-氯-2-甲氧基苯甲酰胺）砜酰胺 - 金属盐; 和（iv）使由式5表示的金属与环己基异氰酸酯或苯基环己基氨基甲酸酯反应，形成由式1表示的格列本脲。
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公开(公告)号：KR1020010111771A
公开(公告)日：2001-12-20
申请号：KR1020000032436
申请日：2000-06-13
Applicant: 한국화학연구원
IPC: A01N43/76
CPC classification number: A01N43/76 , C07D263/58
Abstract: 본 발명은 제초활성이 우수한 다음 화학식 1로 표시되는 페녹시프로피온 아미드 화합물과 벼농사에서 발생하는 피 방제하는 방법, 그리고 이들 화합물을 포함하는 제초제 조성물에 관한 것이다.
상기 화학식 1에서 :
R은 수소원자, 또는 메틸기를 나타내고; X는 수소원자, 또는 플루오로원자를 나타내고; W는 술폰기(-SO
2 -), 카르보닐기(-CO-), 또는 (CH
2 )
n (이때 n은 0 또는 1의 정수임)을 나타내고; R
1 과 R
2 는 서로 같거나 다른 것으로서 수소원자, C
1 ∼C
6 의 알킬기, C
3 ∼C
6 의 싸이클로알킬기, C
1 ∼C
4 의 알콕시기, C
2 ∼C
6 의 알케닐기, 또는 C
2 ∼C
6 의 알키닐기를 나타낸다.-
公开(公告)号：KR1020010038273A
公开(公告)日：2001-05-15
申请号：KR1019990046192
申请日：1999-10-23
Applicant: 한국화학연구원
IPC: C07C51/29
Abstract: PURPOSE: A process for preparing alpha-ketocarboxylic acid derivatives by reacting alpha-hydroxycarboxylic acid derivatives with hypobromous acid(HOBr) is provided, which is industrially useful by using hypobromous acid in place of an oxidant that is expensive and harmful to environment. CONSTITUTION: The titled alpha-ketocarboxylic acid derivatives of formula 1 is prepared by reacting alpha-hydroxycarboxylic acid derivatives with hypobromous acid as an oxidant at -5 to 40deg.C, wherein the hypobromous acid is used in the range of 1 to 2 molar equivalent based on the compound of formula 2.
Abstract translation: 目的：提供通过使α-羟基羧酸衍生物与次溴酸（HOBr）反应制备α-酮羧酸衍生物的方法，其通过使用次溴酸代替昂贵且对环境有害的氧化剂在工业上是有用的。 构成：式1-5的标题α-酮羧酸衍生物通过α-羟基羧酸衍生物与次溴酸作为氧化剂在-5至40℃下反应制备，其中次溴酸的使用量为1至2摩尔当量 基于式2的化合物。
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公开(公告)号：KR100252461B1
公开(公告)日：2000-04-15
申请号：KR1019970050283
申请日：1997-09-30
Applicant: 한국화학연구원
IPC: C07B39/00
Abstract: PURPOSE: A method for preparing carboxylic chloride compounds whose chloride is substituted from the lactone compound is provided, to improve the production yield with lowering the reaction temperature. CONSTITUTION: The method comprises the steps of reacting lactone compound and thionyl chloride in the presence of a Lewis acid and a quaternary ammonium salt at the atmospheric pressure and at 90-100 deg.C, wherein the addition amounts of the Lewis acid, the quaternary ammonium salt and thionyl chloride are 0.1-20 mol%, 0.1-20 mol% and 1-10 equivalence based on the amount of the lactone compound, respectively. Preferably the lactone compound is represented by the formula 2a or 2b, wherein R1, R2, R3 and R4 are H, a halogen atom, an alkyl group of C1-C4 or a haloalkyl group of C1-C4; R5 is H or an alkyl group of C1-C4; and n is an integer of 1-6. Preferably the Lewis acid is selected from MgCl2, MgBr2, SnCl2, SnCl4, TiCl4, AlCl3, FeCl3, BF3Et2O, BCl3, B(OEt)3, B(OMe)3 and B(O-iPr)3.
Abstract translation: 目的：提供一种制备氯化物由内酯化合物取代的氯化物化合物的方法，以降低反应温度来提高产率。 方案：该方法包括在大气压和90-100℃下在路易斯酸和季铵盐存在下使内酯化合物和亚硫酰氯反应的步骤，其中路易斯酸，季铵 铵盐和亚硫酰氯分别为0.1-20摩尔％，0.1-20摩尔％和1-10当量，基于内酯化合物的量。 优选内酯化合物由式2a或2b表示，其中R1，R2，R3和R4是H，卤素原子，C1-C4烷基或C1-C4卤代烷基; R5是H或C1-C4的烷基; n为1-6的整数。 路易斯酸优选选自MgCl 2，MgBr 2，SnCl 2，SnCl 4，TiCl 4，AlCl 3，FeCl 3，BF 3 Et 2 O，BCl 3，B（OEt）3，B（OMe）3和B（O-iPr）3。
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公开(公告)号：KR100245015B1
公开(公告)日：2000-03-02
申请号：KR1019970050282
申请日：1997-09-30
Applicant: 한국화학연구원
IPC: C07C303/02 , C07C303/18 , C07C303/24
Abstract: 본 발명은 ο-(카르보알콕시)페닐메탄술포닐 클로라이드 유도체의 제조방법에 관한 것으로서, 더욱 상세하게는 ο-(클로로메틸)벤조산 에스테르로부터 중간체 화합물으로서 ο-(카르보알콕시)페닐메탄티오술폰산염을 합성한 다음, 염소화반응시켜 술포닐우레아 제초제 합성에 중요한 화합물인 다음 화학식 1로 표시되는 ο-(카르보알콕시)페닐메탄술포닐 클로라이드 유도체를 제조하는 새로운 방법에 관한 것이다.
[화학식 1]
상기 화학식 1에서 : R
1 은 수소원자, 할로겐원자, 니트로기, C
1 ∼C
4 의 알킬기 또는 C
1 ∼C
4 의 할로알킬기를 나타내고; R
2 는 C
1 ∼C
6 의 알킬기 또는 C
3 ∼C
6 의 사이클로알킬기를 나타낸다.
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