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Optimization of reaction conditions for the unsubstituted 2-aminoquinazoline derivatives.
| ||||
|---|---|---|---|---|
| entry | acid/base | equivalent | solvent | yields (%)c |
| 1 | PTSA | 1 | THF | 61 |
| 2 | PTSA | 1 | DMF | 75 |
| 3 | KOtBu | 0.5 | DMF | 55 |
| 4 | KOtBu | 1 | DMF | 65 |
| 5a | PTSA | 1 | DMF | 8 |
| 6b | PTSA | 1 | DMF | 0 |
Reaction Carried out at 70° C.
Reaction carried out at room temperature.
Isolated yields (flash chromatography). PTSA: para toluene sulfonic acid
