反应详情

温度

150 °C

Degassed THF/H2O (4 mL, 10:1) was added to a microwave vial containing 2-(4-bromophenyl)-3-methyl-4-oxo-N-(pyridin-2-yl)-3,4-dihydroquinazoline-8-carboxamide 28 (100 mg, 0.23 mmol), Cs2CO3 (224 mg, 0.69 mmol), Pd(OAc)2 (1.5 mg, 0.007 mmol), XPHOS (65 mg, 0.014 mmol), and potassium 1-trifluoroboratomethylpyrrolidine (48 mg, 0.25 mmol). The reaction mixture was heated at 150° C. in a microwave reactor for 30 min., poured into H2O and extracted with EtOAc. The combined organics were washed with brine, dried, concentrated and the crude residue purified by MPLC eluting with CH2Cl2/MeOH (0-10%) to give Compound 275 (63 mg, 63% yield). MS (ESI) calc. for C26H25N5O2: 439.20. found: 440 [M+H].

1. customDegassed THF/H2O (4 mL, 10:1)
2. additionwas added to a microwave
3. extractionextracted with EtOAc
4. washThe combined organics were washed with brine
5. customdried
6. concentrationconcentrated
7. customthe crude residue purified by MPLC
8. washeluting with CH2Cl2/MeOH (0-10%)