Table 1. Screening of Solvents Using α,α-Difluoro-β-ketoester 2a.

| entry | solvent | temp. (°C) | isolated yield of 4aa (%) | 19F NMR yield of 2a (%) | 19F NMR yield of 5 (%) |
|---|---|---|---|---|---|
| 1 | DMSO | 150 | 20 | 0 | 34 |
| 2 | DMF | 150 | 13 | 0 | 50 |
| 3 | NMP | 150 | 25 | 0 | 40 |
| 4 | DMA | 150 | 0 | 0 | 51 |
| 5 | toluene | reflux | 0 | 94 | 0 |
| 6 | THF | reflux | 20 | 48 | 7 |
| 7 | CH3CN | reflux | 42 | 35 | 0 |