Table 5.
Use of Substituted Heteroaryls as Electrophiles in the One-Pot Miyaura Borylation/Suzuki Cross-Coupling Reaction Utilizing BBA and XPhos-Pd-G2
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General conditions: a) 1 mol % XPhos-Pd-G2, 2 mol % XPhos, 3.0 equlv KOAc, 3.0 equiv B2(OH)4, EtOH (0.1 M), 80 °C for time indicated, b) 3 equiv 1.8 M K2CO3. 1 equiv second halide. 80 °C, 15 h.
1.3 equiv halide added in second step.
< 5% transesterification observed.
