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    • 6. 发明公开
    • 아크리디늄 화합물 및 이를 이용한 화학발광 조성물
    • 化合物和使用该化合物的亮片组合物
    • KR1020020051328A
    • 2002-06-29
    • KR1020000080108
    • 2000-12-22
    • 백운필한태희한영필김병효
    • 백운필김병효한영필한태희
    • C09K11/07
    • C09K11/07C07D219/04C09K2211/1018G01N33/582
    • PURPOSE: Provided are an acridinium compound, which is used as a chemiluminescent agent and excellent in luminescent efficiency and stability, and a chemiluminescent composition using the acridinium compound. CONSTITUTION: The acridinium compound is represented by the formula 1, wherein R1 is methyl or benzyloxy carbonyl ethyl, X is carbon or nitrogen, R2 and R3 are hydrogen, fluoro, methyl, or nitro, R4 is hydrogen, fluoro, methyl, or benzyloxy carbonyl ethyl, and n is 1 or 2. And the chemiluminescent composition comprises 1'-methyl pyridine-4'-yl acridine-9-carboxylate trifluoromethane sulfonate and 1'-methyl pyridine-4'-yl 10-acridinium-9-carboxylate di(trifluoromethane sulfonate) in the weight ratio of 1:2.5.
    • 目的:提供用作化学发光剂并且发光效率和稳定性优异的吖啶鎓化合物和使用吖啶鎓化合物的化学发光组合物。 构成:吖啶鎓化合物由式1表示,其中R1是甲基或苄氧基羰基乙基,X是碳或氮,R2和R3是氢,氟,甲基或硝基,R4是氢,氟,甲基或苄氧基 羰基乙基,n为1或2.化学发光组合物包含1'-甲基吡啶-4'-基吖啶-9-羧酸三氟甲磺酸酯和1'-甲基吡啶-4'-基10-吖啶-9-羧酸酯 二(三氟甲烷磺酸盐)重量比为1:2.5。
    • 7. 发明公开
    • N-[2-(디메틸아미노)에틸]아크리딘-4-카복스아미드의 제조 방법
    • 制备N- [2-(二甲基氨基)乙基]亚胺-4-羧酰胺的方法
    • KR1020000049239A
    • 2000-07-25
    • KR1019997003343
    • 1997-10-17
    • 제노바 리미티드
    • 데니윌리암알렉산더가마지스와르날라타아쿠라티야스파이서쥴리앤라이트마이클하이만데이비드프랑크
    • C07D219/04
    • C07D219/04C07C227/18C07C229/58
    • PURPOSE: A process for the production of the anti-cancer drug N-£2-(dimethylamino)ethyl|acridine-4-carboxamide and derivatives thereof is provided. CONSTITUTION: An acridine carboxamide is represented by formula (I) wherein each of R1, R2, R5 and R6, which can be the same or different, is hydrogen or an organic substituent, x is an integer of 1 to 6 and Y is N(R)2 wherein R is C1-C6 alkyl. The process comprises: (a) cyclizing a compound of formula (II) wherein R1, R2, R5 and R6 are as defined above and R3 is C1-C6 alkyl, aryl or aryl-C1-C3 alkyl, by treatment with a Lewis acid in an organic solvent, to obtain a compound of formula (III) wherein R1, R2, R3, R5 and R6 are as defined above; (b) treating either (i) the compound of formula (III) as defined above with a primary alkylamine of the formula (IV): NH2(CH2)xY, wherein x and Y are as defined above; or (ii) the carboxylic acid, obtainable by hydrolysing the compound of formula (III) as defined above under basic conditions, with a primary alkyl amine of formula (IV) as defined above in the presence of a suitable coupling agent to obtain a compound of formula (I) as defined above; and (c) if desired, converting one compound of formula (I) into another compound of formula (I), and/or converting a compound of formula (I) into a pharmaceutically acceptable salt thereof. The aldehyde of formula (II) is obtained by oxidation of the corresponding alcohol, which in turn is produced by mild reduction of the corresponding carboxylic acid via an immidazolide intermediate.
    • 目的:提供生产抗β-药物N-(2-氨基乙基)乙基吖啶-4-甲酰胺及其衍生物的方法。 构成:吖啶甲酰胺由式(I)表示,其中可以相同或不同的R 1,R 2,R 5和R 6各自为氢或有机取代基,x为1至6的整数,Y为N (R)2,其中R是C 1 -C 6烷基。 该方法包括:(a)通过用路易斯酸处理使环,其中R 1,R 2,R 5和R 6如上定义并且R 3是C 1 -C 6烷基,芳基或芳基-C 1 -C 3烷基的式(II)化合物 在有机溶剂中,得到其中R 1,R 2,R 3,R 5和R 6如上定义的式(III)化合物; (b)用式(IV)的伯烷基胺:NH 2(CH 2)x Y(其中x和Y如上定义)处理(i)如上定义的式(III)化合物; 或(ii)通过在碱性条件下将上述式(Ⅳ)化合物与上述式(Ⅳ)的伯烷基胺在合适的偶合剂存在下水解得到的羧酸,得到化合物 的式(I)定义; 和(c)如果需要,将一种式(I)化合物转化为另一种式(I)化合物,和/或将式(I)化合物转化为其药学上可接受的盐。 通过氧化相应的醇获得式(II)的醛,其依次通过咪唑啉中间体温和还原相应的羧酸而产生。