Table 1. Optimization of the reaction conditions a .
| ||||
| # | Base (0.1 eq.) | Solvent | Temp./time | Yield (%) |
| 1 | Cs2CO3 | DMSO | 30 °C/6 h | 90 b |
| 2 | Cs2CO3 | DMSO | 80 °C/1 h | 87 |
| 3 | Cs2CO3 | DMSO | 100 °C/1 h | 96 |
| 4 | KOH | DMSO | 100 °C/0.5 h | 96 (92 c ) |
| 5 | K2CO3 | DMSO | 100 °C/1 h | 82 |
| 6 | NEt3 | DMSO | 100 °C/1 h | 0 |
| 7 | KOH | DMF | 100 °C/0.5 h | 60 |
| 8 | KOH | MeCN | 100 °C/0.5 h | 55 |
| 9 | KOH | EtOH | 100 °C/0.5 h | 35 |
| 10 | Cs2CO3 | EtOH | 100 °C/0.5 h | 0 |
aConditions: 1a (1.15–1.25 mmol), 3a (1 mmol), solvent (2 mL); microwave heating, sealed tube; isolated yield.
bWorkup with aq. HCl (1 M).
c 3a (5 mmol).