Sequential Direct SNAr Reactions of Pentafluorobenzenes with Azole or Indole Derivatives

被引:33
作者
Diness, Frederik [1 ]
Begtrup, Mikael [1 ]
机构
[1] Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark
关键词
ARYLATION; SUBSTITUTION; FLUORINE;
D O I
10.1021/ol5012554
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Sequential regioselective N-arylations through high-yielding catalyst-free direct SNAr reactions of pentafluor-obenzene derivatives with azole or indole derivatives are described. The N-arylated derivatives were further functionalized through a microwave-assisted cross-coupling reaction via C-H bond activation or Suzuki conditions. The order of the reactions could be reversed, proving full orthogonality between the reactions which led to well-defined fully substituted benzene derivatives.
引用
收藏
页码:3130 / 3133
页数:4
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