Table 3. Use of Different Lewis Acid and Lewis Base by Microwave Irradiation (M.W) For Compound 4.
entry | cat (mol %) | conditionsb | yield (%)a |
---|---|---|---|
1 | no catalyst no M.W | water/ethanol, 1 day | trace |
2 | no catalyst | water/ethanol, 1 h | 45 |
3 | AlCl3 (15) | water/ethanol, 3 min | 49 |
4 | MgCl2 (15) | water/ethanol, 3 min | 47 |
5 | FeCl3·6H2O (15) | water/ethanol, 3 min | 56 |
6 | Fe(OTf)3 (15) | water/ethanol, 3 min | 69 |
7 | ZnBr2 (15) | water/ethanol, 3 min | 74 |
8 | CuCl2 (15) | water/ethanol, 3 min | 66 |
9 | PdCl2 (15) | water/ethanol, 3 min | 87 |
10 | Pd(OAC)2(15) | water/ethanol, 3 min | 89 |
11 | p-TsOH (15) | water/ethanol, 3 min | 75 |
12 | Et3N (15) | water/ethanol, 3 min | 67 |
13 | TBABrc (15) | water/ethanol, 3 min | 66 |
14 | TiCl4 (15) | water/ethanol, 3 min | 71 |
15 | l-Proline (15) | water/ethanol, 3 min | 84 |
16 | Cys (15) | water/ethanol, 3 min | 98 |
17 | Cys (15) | ||
No M.W | water/ethanol, 3 min | 88 |
Isolated yields based on 4.
Reaction conditions: 1 (1 mmol), 2a (1.5 mmol), and 3a (1 mmol) in a mixture of water and ethanol (3:1 ratio) by microwave irradiation conditions, 3 min.