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Synthesis of polyfluorinated o-hydroxyacetophenones – convenient precursors of 3-benzylidene-2-phenylchroman-4-ones
Journal of Fluorine Chemistry ( IF 1.7 ) Pub Date : 2019-11-25 , DOI: 10.1016/j.jfluchem.2019.109435
Larisa Politanskaya , Evgeny Tretyakov , Chanjuan Xi

A simple and efficient approach to the synthesis of fluorinated o-hydroxyacetophenones in good to excellent yields is reported. We demonstrated a convenient method for replacing the iodine atom in o-iodophenols with MeC(=O)– group through the introduction and subsequent hydrolysis of TIPS–C≡C– moiety by of p-toluenesulfonic acid monohydrate. The resulting compounds may serve as precursors for the synthesis of polyfluorinated 3-benzylidene-2-phenylchroman-4-one derivatives that are of interest as objects for the evaluation of their pharmacological properties.



中文翻译:

多氟邻羟基苯乙酮的合成-3-亚苄基-2-苯基苯并吡喃-4-酮的便利前体

据报道,一种简单有效的合成氟化羟基苯乙酮的方法,收率很好。我们介绍了一种简便的方法,该方法是通过引入和随后用甲苯磺酸一水合物水解TIPS-C≡C-部分来用MeC(= O)-基团替换碘苯酚中的碘原子。所得化合物可以用作合成多氟化3-亚苄基-2-苯基苯并二氢-4-酮衍生物的前体,这些衍生物作为评估其药理性质的目的而受到关注。

更新日期:2019-11-26
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