共 28 条
Sequential Direct SNAr Reactions of Pentafluorobenzenes with Azole or Indole Derivatives
被引:33
作者:

Diness, Frederik
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机构:
Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark

Begtrup, Mikael
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Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark
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.
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页码:3130 / 3133
页数:4
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