Table 4. Screening of Basic Conditions for Post-cyclization.
| entry | catalyst | conc. (equiv) | time (h) | yield (%)a |
|---|---|---|---|---|
| 1 | DIPEA | 0.1 | 1 | 20 |
| 2 | DIPEA | 0.1 | 12 | 25 |
| 3 | NaOCH3 | 0.1 | 1 | 33 |
| 4 | NaOCH3 | 0.1 | 12 | 40 |
| 5 | NaOCH3 | 1 | 1 | 86 |
| 6 | NaOCH3 | 2 | 1 | 80 |
Isolated yield.
| entry | catalyst | conc. (equiv) | time (h) | yield (%)a |
|---|---|---|---|---|
| 1 | DIPEA | 0.1 | 1 | 20 |
| 2 | DIPEA | 0.1 | 12 | 25 |
| 3 | NaOCH3 | 0.1 | 1 | 33 |
| 4 | NaOCH3 | 0.1 | 12 | 40 |
| 5 | NaOCH3 | 1 | 1 | 86 |
| 6 | NaOCH3 | 2 | 1 | 80 |
Isolated yield.