Selected optimization details for the trifluoromethylarylation.
| ||
|---|---|---|
| Entry | Deviation from optimized conditions | Isolated yield, 4a (%) |
| 1 | None | 72% |
| 2 | HFIP (0.2 M) at 40 °C | 67% |
| 3 | HFIP (0.2 M) at rt | 58% |
| 4 | HFIP (0.2 M) at 80 °C | 53% |
| 5 |
instead of 3 |
34% |
| 6 |
instead of 3 |
nr |
| 7 |
and CF3SO2Na instead of 3 |
nr |
| 8 | CH2Cl2, CH3CN or AcOH (0.2 M) at rt | nr |
| 9 | TFE (0.2 M) at rt | 11% |
| 10 | 2.0 equiv. of 1a | 65% |
| 11 | 2.0 equiv. of 2a | 63% |
| 12 | 2.0 equiv. of 3 | 22% |
instead of 3
instead of 3
and CF3SO2Na instead of 3