Synthesis of Fmoc-protected Q4As via imidazolidinones 3.
R= | X= | 3, yield | (S)-4, yield/% (scale) |
---|---|---|---|
H | 4-Br | 3a, 94 | 4a, 83 (1.8 g) |
H | 3-Br | 3b, 91 | 4b, 50 (1.5 g) |
H | 3-CN | 3c, 83 | |
H | 3,5-F2 | 3d, 91 | 4d, 67 (0.5 g) |
H | 3,5-Cl2 | 3e, 90 | |
Ph | 4-Cl | 3f, 89 | 4f, 51 (0.2 g) |
Ph | 4-Me | 3g, 80 | 4g, 62 (0.4 g) |
Ph | 3-Br | 3h, 95 | 4h, 50 (0.4 g) |
4-BnOC6H4 | 4-Me | 3i, 88 | |
4-BnOC6H4 | 3-F, 4-Br | 3j, 93 |