首页> 外国专利> Method for preparing canagliflozin intermediate 2-(2-methyl-5-bromobenzyl)-5-(4-fluorophenyl)thiophene

Method for preparing canagliflozin intermediate 2-(2-methyl-5-bromobenzyl)-5-(4-fluorophenyl)thiophene

机译:卡格列净中间体2-(2-甲基-5-溴苄基)-5-(4-氟苯基)噻吩的制备方法

摘要

Provide in the present invention is a method for preparing canagliflozin intermediate 2-(2-methyl-5-bromobenzyl)-5-(4-fluorophenyl)thiophene. The method comprises a compound, shown as formula (II), of (5-bromo-2-methylphenyl)[5-(p-fluorophenyl)thiophene-2-yl]ketone being reduced under the action of a directly used borane solution or borane locally produced by reacting alkali metal borohydride with a Lewis acid in a suitable solvent and at a suitable temperature, so as to obtain the compound of formula (I) of 2-(2-methyl-5-bromobenzyl)-5-(4-fluorophenyl)thiophene. The preparation method avoids the use of expensive reductive agents and guarantees the complete conversion of raw materials, wherein the post-treatment is simple, the purity of product obtained is high, the reaction yield is high, in the preparation method is simple and convenient, and can easily be used in industry.
机译:本发明提供了一种制备卡格列净中间体2-(2-甲基-5-溴苄基)-5-(4-氟苯基)噻吩的方法。该方法包括如式(II)所示的在直接使用的硼烷溶液的作用下还原的(5-溴-2-甲基苯基)[5-(对氟苯基)噻吩-2-基]酮的化合物。通过在合适的溶剂中和合适的温度下使碱金属硼氢化物与路易斯酸反应而局部产生的硼烷,以获得2-(2-甲基-5-溴苄基)-5-(4)的式(I)化合物-氟苯基)噻吩。该制备方法避免了昂贵的还原剂的使用,并保证了原料的完全转化,后处理简单,所得产物的纯度高,反应产率高,制备方法简单方便。并且可以很容易地在工业中使用。

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