Table 4.
# 1–6 from Table 1 | Penalty |
1 Yield: 83% | 9 |
2 Formamide (1 mL) | 0 |
Pd(OAc)2 (0.038 mmol, 8.5 mg) | 0 |
dppf (0.038 mmol, 21.1 mg) | 0 |
Imidazole (0.75 mmol. 51.1 mg) | 0 |
KOBu-t (1.13 mmol, 126 mg) | 0 |
3 Bromobenzene (N) | 5 |
Formamide (T) | 5 |
KOBu-t (F) | 5 |
dppf (T) | 5 |
4 Microwave activation | 2 |
Nitrogen atmosphere | 1 |
5 180°C, 400 s | 2 |
6 Cooling | 0 |
Dilution with EtOAc | 0 |
Washing with water and brine | 3 |
Drying over potassium carbonate | 0 |
Removal of EtOAc | 0 |
Silica gel chromatography | 10 |
Penalty points total: | 47 |