Table 1.
Entry | R1 | R2 | Comp. | Yield (%)a | CLogP | tPSA |
---|---|---|---|---|---|---|
1 | Cyclopropyl | 2-thienyl | 7a | 82 | 3.799 | 52.65 |
2 | iBu | 2-thienyl | 7b | 52 | 4.8955 | 52.65 |
3 | iBu | 2-furanyl | 7c | 72 | 4.0715 | 61.88 |
4 | 2-BrC6H4 | 2-furanyl | 7d | 63 | 7.5791 | 52.65 |
5 | 2-BrC6H4 | Acetyl | 7e | 75 | 4.672 | 52.65 |
6 | 2-BrC6H4 | 3-pyridyl | 7f | 71 | 5.5395 | 65.01 |
7 | iBu | 3-pyridyl | 7g | 72 | 3.7945 | 65.01 |
8 | iBu | 2-COOHC6H4 | 7h | 76 | 4.9034 | 89.95 |
9 | Bzl | Ph | 7i | 62 | 6.0965 | 52.65 |
10 | Ph | Ph | 7j | 71 | 6.2375 | 52.65 |
11 | Phenethyl | 4-pyridyl | 7k | 67 | 4.4345 | 65.01 |
12 | H | Ph | 7l | 66 | 3.8747 | 61.44 |
13 | 2-BrC6H4 | 2-furanyl | 7m | 76 | 5.8165 | 61.88 |
14 | 2-BrC6H4 | methyl | 7n | 78 | 3.5115 | 52.65 |
Isolated yield (%) from the one-pot procedure.