Table 1.
Direct arylation and subsequent allylation.
| ||||||
|---|---|---|---|---|---|---|
| Entry | X | R1 | Product | Yield (%) | Product | Yield (%) |
| 1 | O | 4-OMOM | 18a | 60% | 16a | 69% |
| 2 | O | 4-OH | 18b | n.s. | 16b | 91% 1 |
| 3 | O | 4-OMe | 18c | 58% | 16c | 70% |
| 4 | O | 3,5-dimethoxy | 18d | 51% | 16d | 66% |
| 5 | O | H | 18e | 44% | 16e | 74% |
| 6 | O | 4-F | 18f | 41% | 16f | 72% |
| 7 | O | 4-CHF2 | 18g | 45% | 16g | 69% |
| 8 | O | 2-Cl | 18h | 44% | 16h | 51% |
| 9 | S | 4-OMOM | 22a | 58% | 23a | 46% |
| 10 | S | 4-OMe | 22c | 31% | 23c | 58% |
n.s. not synthesized; 1 via MOM-deprotection from 16a, the yield refers only to the deprotection step.