反应详情

(S)—N-(4-fluorobenzyl)-6-bromo-4-(tetrahydrofuran-3-yloxy)quinazolin-2-amine (50 mg, 0.12 mmol), potassium carbonate (33 mg, 0.24 mmol), tetrakis(triphenyl-phosphine)palladium (8 mg, 0.007 mmol) and 4-((2-(dimethylamino)ethyl)-carbamoyl)phenylboronic acid (36 mg, 0.132 mmol) in DMF (1.0 mL) and water (0.3 mL) was heated to 150° C. for 10 minutes under microwave irradiation. Solvents were concentrated in vacuo and the residue was purified by RP HPLC, using a C18 column with a gradient of 0.1% H2O, 0.1% TFA-acetonitrile, to provide the desired product (41 mg) which was characterized by its mass spectrum as follows: MS (m/z): 530 ([M+H]+, 100); HPLC Rt=1.26 minutes (Method B).

1. concentrationSolvents were concentrated in vacuo
2. customthe residue was purified by RP HPLC