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Mild copper-catalyzed N-arylation of azaheterocycles with aryl halides |
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| Authors: | Mark Kuil Gerben M. Visser Jan Willem Terpstra Piet W.N.M. van Leeuwen |
| Affiliation: | a Van ‘t Hoff Institute for Molecular Sciences, Nieuwe Achtergracht 166, 1018 WV Amsterdam, The Netherlands b Laboratory of Organic Chemistry, Wageningen University, Dreijenplein 8, 6703 HB Wageningen, The Netherlands c Solvay Pharmaceuticals, postbus 900, 1380 DA Weesp, The Netherlands |
| Abstract: | A highly efficient copper(I)-catalyzed N-arylation of azaheterocycles with various aryl halides is reported. The N-arylation reaction can be carried out using as low as 0.5 mol % of (Cu(I)OTf)2·PhH and 1.0 mol % of 4,7-dichloro-1,10-phenanthroline as the ligand. Furthermore, cheap and stable copper precursors like Cu(I)I and Cu(II)(OAc)2·H2O and the cheap and mild base K2CO3 can be used. |
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