作者:Haiwen Xiao、Zhonglin Liu、Haigen Shen、Benxiang Zhang、Lin Zhu、Chaozhong Li
DOI:10.1016/j.chempr.2019.02.006
日期:2019.4
Direct trifluoromethylation of C(sp3)–H bonds, especially in late stages, remains a formidable challenge. Herein, we describe the copper-catalyzed benzylic C(sp3)–H trifluoromethylation. With Cu(I) or Cu(II) as the catalyst, (bpy)Zn(CF3)2 (bpy = 2,2′-bipyridine) as the CF3 source, and NFSI (or Selectfluor) as the oxidant, site-selective benzylic C(sp3)–H trifluoromethylation is successfully implemented
C(sp 3)–H键的直接三氟甲基化,尤其是在后期阶段,仍然是一个艰巨的挑战。在这里,我们描述了铜催化的苄基C(sp 3)–H三氟甲基化。以Cu(I)或Cu(II)为催化剂,以(bpy)Zn(CF 3)2(bpy = 2,2'-联吡啶)作为CF 3源,以NFSI(或Selectfluor)作为氧化剂选择性苄基C(sp 3)–H三氟甲基化已在温和条件下成功高效地实施。该协议不仅展示了广泛的底物范围和广泛的官能团兼容性,而且还允许对天然产物或药物衍生物进行有效的后期C(sp 3)–H三氟甲基化。