反应详情

温度

90 °C

(S)-ethyl 2-(2-bromo-7-(4-chlorophenyl)-5-methylbenzo[d]thiazol-6-yl)-2-tert-butoxyacetate (500 mg, 1.01 mmol), tetrakis(triphenylphosphine)palladium(0) (174 mg, 0.15 mmol), lithium chloride (128 mg, 3.02 mmol), and copper(I) iodide (58 mg, 0.3 mmol) were taken in a microwave vial, and the vial was vacuum pumped and flushed with argon three times. To this mixture was added 2-(tributylstannyl)-4-chloropyrimidine (447 mg, 1.11 mmol) in dioxane (12 mL) and the resulting mixture was stirred at 90° C. for 18 h. The reaction mixture was then cooled, filtered through Celite (ethyl acetate eluent), and concentrated. Purification by flash column chromatography on silica gel (hexanes/ethyl acetate eluent) provided the product. LCMS-ESI+ calc'd for C26H26Cl2N3O3S (M+H+): 530.1; Found: 530.0 (M+H+).

1. customflushed with argon three times
2. temperatureThe reaction mixture was then cooled
3. filtrationfiltered through Celite (ethyl acetate eluent)
4. concentrationconcentrated
5. customPurification by flash column chromatography on silica gel (hexanes/ethyl acetate eluent)
6. customprovided the product