A General Catalyst for the β-Selective C–H Bond Arylation of Thiophenes with Iodoarenes


  • We thank Dr. Yasutomo Segawa and Hiromi Sekizawa for experimental assistance and fruitful discussions. This research was supported by a Grant-in-Aid for Scientific Research from MEXT and the JSPS. K.U. and S.Y. thank the JSPS for predoctoral fellowships.


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Open access: The normally less-reactive β position of thiophenes was previously inaccessible to direct functionalization. However, the β selectivity observed with the catalytic system PdCl2/P{OCH(CF3)2}3/Ag2CO3 in the arylation of thiophenes with iodoarenes (see scheme) is a remarkably general phenomenon applicable to unsubstituted, monosubstituted, and disubstituted thiophene derivatives, as well as thiophene-containing fused aromatic compounds.