Table 1 Optimization of reaction conditions
From: The development of an effective synthetic route of lesinurad (RDEA594)
Entry | Solvent | Temperature (°C) | Time | Yield % |
|---|---|---|---|---|
1 | DCM | 25 | 15 h | 81.7 |
2 | DCM | 25 | 12 h | 83.6 |
3 | DCM | 25 | 6 h | 60.4 |
4 | THF | 25 | 12 h | 78.1 |
5 | THF | 120 | 12 h | 70.9 |
6 | DMF | 25 | 12 h | 78.2 |
7 | DMF | 120 | 12 h | 50.4 |
8 | DMF | 120 (microwave) | 30 min | 0a |