Table 2.
entry | deviations from standard conditions | % yield (3a; 3b) | |
---|---|---|---|
1 | none | 10; | 52 |
2 | RuPhos-Pd-G4 | 60; | 12 |
3 | CataCXium A-Pd-G4 | 13; | 49 |
a4 | QPhos-Pd-G3 | —; | 20 |
a5 | RuPhos-Pd-G4, p-benzoquinone (10 mol%) | 43; | 9 |
a6 | w/ p-benzoquinone (10 mol%) | 10; | 50 |
a7 | K2CO3 instead of Cs2CO3 | returned 2a | |
a8 | Phl instead of PhBr | 5; | 15 |
NMR yield based on 1H NMR integration using 1,3,5-trimethoxybenzene as the internal standard. Reactions run on a 0.1 mmol scale.