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|---|---|---|---|---|---|---|
| Entry | Reagent | Solvent | Temp. [°C] | Time [h] | Yieldb [%] | |
| 4a | 5a | |||||
| 1 | K2CO3 | THF | r.t. | 4 | 97 | — |
| 2 | Pyridine | THF | 70 | 12 | Trace | — |
| 3 | — | AcOH | 110 | 3 | 98 | — |
| 4 | PPTS | PhCH3 | 110 | 7 | 95 | Trace |
| 5 | TFA | PhCH3 | 110 | 4 | 95 | Trace |
| 6 | p-TsOH | (CF3)2CHOH | r.t. | 0.5 | — | 98 |
The reactions were performed with 2a (0.2 mmol) in 2 ml of solvent.
Isolated yield.
