Potassium Iodide → HCID 24965444, compound

Participants

Reaction Conditions

Reaction Steps

2-(6-(1,4-Diazepan-1-yl)-2-(4-fluoro-3-methoxyphenyl)-4-oxoquinazolin-3(4H)-yl)-N-isopropylacetamide (EXAMPLE 1i) (28 mg, 0.06 mmol), 2-bromoethanol (30 mg, 0.017 mL, 0.24 mmol), potassium carbonate (17 mg, 0.12 mmol,) and potassium iodide (1 mg, 5.99 μmol) were combined in a microwave vial and DMF (1 mL) added. The reaction mixture was heated at 100° C. for 5 min in the microwave. LCMS indicated that the desired product was being formed. Additional 2-bromoethanol (30 mg, 0.017 mL, 0.24 mmol) was added and reaction mixture was heated at 100° C. for a further 5 min in the microwave. Product was purified by preparative LCMS to afford 2-{2-(4-fluoro-3-methoxyphenyl)-6-[4-(2-hydroxyethyl)perhydro-1,4-diazepin-1-yl]-4-oxo-4H-quinazolin-3-yl}-N-isopropylacetamide (EXAMPLE 4q) (4 mg, 7.82 μmol, 13%).

Provenance & Evidence