Research Article

Palladium-Catalyzed C(sp3)-H Arylation of Benzo[b]thiophen-3(2H)-one 1,1-Dioxide

Table 1

Optimization of phosphine ligands.

Entry1LigandYield (%)2

1L160
2L253
3L337
4L447
5L535
6L611
7L739
8L838
9L917
10L10NR
11No ligandNR

1Reaction conditions: 10 mol% of Pd(OAc)2, 20 mol% of ligand, 0.25 mmol of 1a, 0.5 mmol of 1b, 0.75 mmol of KOtBu, and 1 mL of toluene, 110°C, 24 h. 2GC yield.