Ligand stoichiometry effects on the tandem Larock/Buchwald–Hartwig annulation/cyclization.
Entry | Dt-BPF mol% | XPhos mol% | Yielda (%) |
---|---|---|---|
1 | 30 | 0 | 3 |
2 | 25 | 5 | 8 |
3 | 20 | 10 | 10 |
4 | 15 | 15 | 72 |
5 | 10 | 20 | 64 |
6 | 5 | 25 | 47 |
7 | 0 | 30 | 36 |
Yields were determined by LC/MS using 1,3,5-trimethoxy benzene as an internal standard.