Table 1. Two-step synthesis of aminopyrazoles A.1–28 a .
| ||
| Compound | –R | Overall yield (%) |
| A.1 | H | 69 |
| A.2 | 2-NO2 | 38 |
| A.3 | 3-NO2 | 48 |
| A.4 | 4-NO2 | 16 |
| A.5 b | 2-Br | 35 |
| A.6 | 3-Br | 56 |
| A.7 | 4-Br | 44 |
| A.8 b | 2-Cl | 35 |
| A.9 | 3-Cl | 51 |
| A.10 | 4-Cl | 38 |
| A.11 b | 2-F | 48 |
| A.12 | 3-F | 32 |
| A.13 | 4-F | 38 |
| A.14 b | 2-I | 44 |
| A.15 b | 3-CF3 | 82 |
| A.16 b | 4-CF3 | 83 |
| A.17 b | 2-CO2tBu | 35 |
| A.18 | 3-CO2tBu | 68 |
| A.19 | 4-CO2tBu | 42 |
| A.20 | 2-OBn | 42 |
| A.21 | 3-OBn | 61 |
| A.22 b | 4-OBn | 18 |
| A.23 b | 2-OMe | 50 |
| A.24 | 3-OMe | 73 |
| A.25 b | 4-OMe | 22 |
| A.26 b | 2-C CH | 31 |
| A.27 | 3-C CH | 77 |
| A.28 | 4-C CH | 44 |
aYields are calculated over two steps.
bHydrazones II.x and pyrazoles A.x are described in the ESI.†