Table 1.
| ||||
---|---|---|---|---|
entry | pdt | R1 | R2 | yield (%)a |
1 | 2a | H | 2-OMe Bn | 71 |
2 | 2b | H | 2,3-Cl CH2Ph | 73 |
3 | 2c | 4-Br | nBu | 90 |
4 | 2d | 4-Br | iBu | 91 |
5 | 2e | 4-Br | PMB | 82 |
6 | 2f | 4-Br | cyclopropyl | 81 |
7 | 2g | 4-Br | propargyl | 94 |
8 | 2h | 5-Cl | Allyl | 94 |
9 | 2i | 5-Cl | PMB | 71 |
10 | 2j | 5-Cl | 3-F Bn | 93 |
11 | 2k | 5-Cl | 2-OMe Bn | 87 |
12 | 2-l | 4-Br | (iPr)CHCO2Me | 93 |
13 | 2m | 4-Br | (iBu)CHCO2Me | 77 |
isolated yield after column chromatography