首页> 外国专利> A method for the production of 5 - fluorine - 2 - methyl - 1 - (p - methyl - sulfinyl benzyl identical) - indene - 3 - acetic acid and their saeureadditionssalzen

A method for the production of 5 - fluorine - 2 - methyl - 1 - (p - methyl - sulfinyl benzyl identical) - indene - 3 - acetic acid and their saeureadditionssalzen

机译:一种5-氟-2-甲基-1-(对-甲基-亚磺酰基苄基相同)-茚3-乙酸的制备方法及其缩醛的合成。

摘要

5-Fluoro-2-methyl-1-(p-methylsulphinylbenzylidene)indenyl-3-acetic acid or its salts are prepared. The said acid is obtained by condensing 5-fluoro-2-methyl-1-R1-benzylindene, where R1 is p-methylthio or p-methylsulphinyl, with glyoxylic acid, its salt or ester to give the corresponding 5-fluoro-2-methyl-1-(p-methylthio- (or methylsulphinyl)benzyl)indenylidene-3-acetic acid, its salt or ester. If R1 is p-methylsulphinyl, the indenylidene compound is isomerised to indenyl-3-acetic acid. If R1 denotes methylthio, then the resulting indenylidene-3-acetic acid is isomerised to 5-fluoro-2-methyl-1-(p-methylthiobenzylidene)indenyl-3-acetic acid and the p-methylthio radical is then oxidised to the p-methylsulphinyl group. However, the oxidation can also be carried out first and the isomerisation subsequently. The said compounds can be used as active agents in anti-inflammatory medicaments.
机译:制备5-氟-2-甲基-1-(对甲基亚磺酰基亚苄基)茚基-3-乙酸或其盐。通过将5-氟-2-甲基-1-R-1-苄基茚(其中R1为对甲硫基或对甲基亚磺酰基)与乙醛酸,其盐或酯缩合,得到相应的5-氟-2-基,得到所述酸。甲基-1-(对甲硫基-(或甲基亚磺酰基)苄基)茚基-3-乙酸,其盐或酯。如果R1是对甲基亚磺酰基,则茚基亚烷基化合物异构化为茚基-3-乙酸。如果R1表示甲硫基,那么将所得的茚二亚甲基-3-乙酸异构化为5-氟-2-甲基-1-(对甲硫基亚苄基)茚基-3-乙酸,然后将对甲硫基氧化为对氨基苯甲酸。 -甲基亚磺酰基。但是,也可以首先进行氧化,然后进行异构化。所述化合物可用作抗炎药物中的活性剂。

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