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铜催化环丙醇的开环三氟甲基及硫三氟甲基化反应

2018-06-27


普渡大学代明骥教授、李勇博士(Yong Li)、叶智识博士(Zhishi Ye)及其合作者首次实现了铜催化的环丙醇的开环三氟甲基及硫三氟甲基化开环反应:以方便易得的环丙醇作为底物,在一价铜催化剂及相应的三氟甲基或硫三氟甲基试剂的条件下,快速合成了β-三氟甲基和硫三氟甲基羰基化合物。该反应条件温和,官能团容忍性良好。亲核三氟甲基试剂或硫三氟甲基试剂对α,β-不饱和羰基化合物的共轭加成比较困难,而该方法学巧妙地利用极性反转的策略,实现了β-三氟甲基和硫三氟甲基羰基化合物的高效构建。随后,作者应用该方法学,快速高效地制备了临床试验期的药物LY2409021

 这一研究成果发表于《Org. Lett.》上。


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