二羟基苯乙酮单酰化衍生物的制备

Preparation of Mono Carbonylate Derivatives of Dihydroxyacetophenone

利胆剂羟基苯乙酮体内药效作用时间较短,而它的二羟基单酰化衍生物则能够解决这个问题,有较长的作用时间。文中通过水相反应和活性硼酸衍生物实现了两种二羟基苯乙酮的单酰化反应,产率最高达99%,区域选择性好。经核磁等分析手段对化合物的结构表征。在研究中,探索了反应当量比,反应时间,反应温度对单酰化产率的影响。

Cholagogue hydroxyacetophenone＇s efficacy in humans＇ body is very short.But it＇s dihydroxyacetophenone derivatives can solve this problem.In this journal mono carbonylations of two kinds of dihydroxyacetophenones are achieved through water phrase reaction and active boron acid derivative.The yield and selectivity is great.The structure of the synthetic products were characterized by H NMR.The influences of reaction equiv ratio,time and temperature on mono carboylation yield were also explored.