论文部分内容阅读
α-芳基烷酸类非甾体消炎药(如布洛芬、萘普生等)由于其疗效确切,副作用小等优点正日益受到重视。使用标题试剂还原性地除去各种α-芳基烷酸酯(或腈、醇)的苄位羟基,是一比较简捷的合成方法。反应只需将底物的正己烷溶液加到6当量的标题试剂中,常温反应24小时即可。收率30~99%。改变配比会引起产物复杂和收率下降。反应区域选择性高,只有苄位羟基能够被除去,而其他官能团(包括非苄位的羟基)很少受影响。
α-Arylalkanoic acid nonsteroidal anti-inflammatory drugs (such as ibuprofen, naproxen, etc.) are gaining more and more attention because of their definite curative effect and small side effects. The reductive removal of the benzylic hydroxyl groups of various alpha-aryl alkanoates (or nitriles, alcohols) using the title reagent is a relatively straightforward synthesis. The reaction is only required to add the substrate n-hexane solution to 6 equivalents of the title reagent at room temperature for 24 hours. Yield 30 ~ 99%. Changing the ratio will lead to product complexity and yield decline. The selectivity of the reaction zone is high, only the benzylic hydroxyl group can be removed, while other functional groups (including the non-benzylic hydroxyl group) are less affected.