Table 2. Screening of Acidic Conditions for Post-cyclization.
| yield
(%)a |
||||
|---|---|---|---|---|
| entry | acid, solvent | amount, time | 6a | 7a |
| 1 | TFA, MeOH | 2 equiv., 18 h | 10 | traces |
| 2 | 6 M aq. HCl | 5 mL, 18 h | 33 | traces |
| 3 | acetyl chloride, MeOH | 2 equiv., 18 h | 36 | 5 |
| 4 | 2 M HCl in MeOH | 5 mL, 4 h | 64 | 6 |
Isolated yield.