Table 1.
Cyclization of the Ugi 4-CR to yield the isoindolone scaffold.
|
|
||||
|---|---|---|---|---|---|
| entry | R(4) | n | Ugi (%) a | entry | cyclisation(%) b |
| 5a |
|
2 | 73 | 6a | 55 |
| 5b |
|
2 | 50 | 6b | 89 |
| 5c |
|
2 | 75 | 6c | 32 |
| 5d |
|
2 | 56 | 6d | 72 |
| 5e |
|
2 | 40 | 6e | 95 |
| 5f |
|
3 | 78 | 6f | 76 |
| 5g |
|
3 | 62 | 6g | 42 |
| 5h |
|
3 | 43 | 6h | 40 |
| 5i |
|
3 | 68 | 6i | 99 |
| 5j |
|
3 | 41 | 6j | 79 |
TFA, CH2Cl2, RT. 1 min.
NaH, THF, RT, 4h