首页> 外国专利> New 7-fluoro-4-(2-(4-(thieno(3,2-c)pyridin-4-yl)piperazin-1-yl)-2-oxoethyl)-quinoleine-2(1H)-one useful as an intermediate to prepare 7-fluoro-2-oxo-4-(2-(4-(thieno(3,2-c)pyridin-4-yl)piperazin-1-yl)ethyl)-1,2-dihydroquinoleine-1-acetamide

New 7-fluoro-4-(2-(4-(thieno(3,2-c)pyridin-4-yl)piperazin-1-yl)-2-oxoethyl)-quinoleine-2(1H)-one useful as an intermediate to prepare 7-fluoro-2-oxo-4-(2-(4-(thieno(3,2-c)pyridin-4-yl)piperazin-1-yl)ethyl)-1,2-dihydroquinoleine-1-acetamide

机译:新的7-氟-4-(2-(4-(噻吩并(3,2-c)吡啶-4-基)哌嗪-1-基)-2-氧代乙基)-喹啉-2(1H)-可用作制备7-氟-2-氧代-4-(2-(4-(硫代(3,2-c)吡啶-4-基)哌嗪-1-基)乙基)-1,2-二氢喹啉的中间体1-乙酰胺

摘要

7-Fluoro-4-[2-[4-(thieno[3,2-c]pyridin-4-yl)piperazin-1-yl]-2-oxoethyl]-quinoleine-2(1H)-one (I) and its salts are new. 7-Fluoro-4-[2-[4-(thieno[3,2-c]pyridin-4-yl)piperazin-1-yl]-2-oxoethyl]-quinoleine-2(1H)-one of formula (I) and its salts are new. Independent claims are included for (1) the preparation of (I); and (2) preparation of 7-fluoro-2-oxo-4-(2-[4-[thieno[3,2-c]pyridin-4-yl)piperazin-1-yl]ethyl]-1,2-dihydroquinoleine-1-acetamide (II) comprising reaction of 3-(acetyloxy)-5-[(3-fluorophenyl)amino]-5-oxopent-2-enoic acid (III) with 4-(piperazin-1-yl)thieno[3,2-c]pyridine (IV) to obtain (I) reduction of (I) and arylation of the obtained reduced compound using an electrophilic agent i.e. an alkyl halide. [Image].
机译:7-氟-4- [2- [4-(噻吩并[3,2-c]吡啶-4-基]哌嗪-1-基] -2-氧代乙基]-喹啉-2(1H)-一(I)它的盐是新的。 7-氟-4- [2- [4-(噻吩并[3,2-c]吡啶-4-基]哌嗪-1-基] -2-氧代乙基]-喹啉-2(1H)-的一个式( I)及其盐是新的。 (1)制备(I)包括独立权利要求; (2)7-氟-2-氧代-4-(2- [4- [噻吩并[3,2-c]吡啶-4-基]哌嗪-1-基]乙基] -1,2-的制备包含3-(乙酰氧基)-5-[(3-氟苯基)氨基] -5-氧opent-2-烯酸(III)与4-(哌嗪-1-基)硫杂环丁酸酯反应的二氢喹油酸-1-乙酰胺(II) [3,2-c]吡啶(IV)用于获得(I)的还原(I),并且使用亲电子试剂即卤代烷将所得的还原化合物芳基化。 [图片]。

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