Table 1. Optimization of the Synthesis of Compound 3aa,ba.
| entry | base | solvent | MW power (W) | irradiation time (min) | % yield 3ac |
|---|---|---|---|---|---|
| 1 | Et3N | CH3CN | 100 | 4 | 60 |
| 2 | Et3N | CH3CN | 100 | 6 | 75 |
| 3 | Et3N | CH3CN | 100 | 8 | 65 |
| 4 | Et3N | CH3CN | 200 | 2 | 60 |
| 5 | Et3N | CH3CN | 200 | 4 | 85 |
| 6 | Et3N | CH3CN | 200 | 6 | 82 |
| 7 | Et3N | CH3CN | 300 | 2 | 65 |
| 8 | Et3N | CH3CN | 300 | 4 | 80 |
| 9 | K2CO3 | CH3CN | 200 | 4 | 92d |
| 10 | Na2CO3 | CH3CN | 200 | 4 | 87 |
| 11 | CaH2 | CH3CN | 200 | 4 | 85 |
| 12 | K2CO3 | DMF | 200 | 4 | 90 |
| 13 | K2CO3 | toluene | 200 | 4 | 90 |
| 14 | K2CO3 | CH3CN | 83e |
Reaction conditions: All of the reactions were carried out on a CEM Discover-300 microwave synthesizer.
Power mode, 50 psi.
Isolated yield.
Optimized condition.
Reflux for 12 h.
