Table 3. Third Series of Quinazoline Derivativesa.
| entry | reagent 1: RNH2 | product (yield %) | reagent 2: R2B(OH)2 | product (yield %) |
|---|---|---|---|---|
| 1 | 4-methylaniline | 8a (53.4) | thiophene-2-boronic acid pinacol ester | 9a (77.0) |
| 2 | 3,4-difluorobenzylamine | 8b (93.2) | 9b (85.3) |
Reagents and conditions: (a) Corresponding aniline or benzylamine, DMAP, Et3N, toluene, reflux, 3 h; (b) thiophene-2-boronic acid pinacol ester, K2CO3, PdCl2(PPh3)2, toluene/dioxane/water (10:5:8, v/v/v), 90 °C, overnight.
