Optimisation of one-pot protocol. Yields were determined by 19F NMR analysis using 1-bromo-4-fluorobenzene as an internal standard.
| ||
|---|---|---|
| Entry | Acid (equiv.) | 4aa (yield%) |
| 1 | AcOH (3) | 85 |
| 2 | AcOH (4) | 75 |
| 3 | AcOH (5) | 72 |
| 4 | PivOH (3) | 1 |
| 5 | iBuCOOH (3) | 71 |
| 6 | TFA (3) | 5 |