不饱和腙类化合物的三氟甲基化反应

氟具有强的吸电子性、亲脂性,将含氟的取代基引入药物中能显著改变药物的药代动力学性质,包括极性、亲脂性、代谢稳定性等,因此向化合物中引入三氟甲基是近期有机合成及医药领域的热点,开发利用经济、高效、绿色的三氟甲基试剂具有重要的意义。以三氟甲烷亚磺酸钠为三氟甲基源,在温和的条件下实现不饱和腙类化合物的三氟甲基化。结果表明,三氟甲烷亚磺酸钠作为三氟甲基源具有良好的反应活性,反应条件温和,符合绿色化学要求,并提供了向不饱和腙类化合物引入三氟甲基的新方法。

Study on Trifluoromethylation of Unsaturated Hydrazone Compounds

Fluorine has strong electron absorption and lipophilicity.The introduction of fluorine-containing substituents into drugs can significantly change the pharmacokinetic properties of drugs,including polarity,lipophilicity,metabolic stability and so on.Therefore,the introduction of trifluoromethyl into compounds is a hot spot in the field of organic synthesis and medical field,and the development and utilization of economical and efficient trifluoromethyl reagents is of great significance.We used sodium trifluoromethanesulfinate as the source of trifluoromethyl to achieve trifluoromethylation of unsaturated hydrazone compounds under mild conditions.The results showed that sodium trifluoromethanesulfinate had the good reactivity as a source of trifluoromethyl,and the reaction conditions were mild,which met the requirements of green chemistry.The research also provided a new method for introducing trifluoromethyl group into unsaturated hydrazone compounds.