Table 1.
Optimization of Reactions Conditions
| ||||
|---|---|---|---|---|
| entry | Cu catalyst | Pd catalyst | 7:8:9 | yield of 7 (%)a |
| 1b | IMesCuCl | Pd-Pt-Bu3-G3 | 3:1:2 | 24 |
| 2b | It-BuCuBr | Pd-Pt-Bu3-G3 | 11:1:<0.1 | 42 |
| 3 | It-BuCuBr | Pd-Pt-Bu3-G3 | 11:1:<0.1 | 57 |
| 4 | It-BuCuBr | Pd-Pt-Bu2CH2t-Bu-G3 | 3:1:< 0.1 | 47 |
| 5 | It-BuCuBr | Pd-QPhos-G3 | 15:1:<0.1 | 77 |
| 6c | It-BuCuBr | Pd-QPhos-G3 | 10:1:<0.1 | 58 |
a
Yield and product ratios determined by 1H NMR analysis of the crude reaction mixture with an internal standard.
b
Reaction run with 1.5 equiv of KOt-Bu instead of 2 equiv.
c
Reaction run with NaOt-Bu instead of KOt-Bu.
