反应详情

温度

100 °C

(S)-methyl 2-(2-bromo-7-(4-chlorophenyl)-5-methylbenzo[d]thiazol-6-yl)-2-tert-butoxyacetate (17.4 mg, 0.036 mmol), Pd(PPh3)4 (2.1 mg, 0.002 mmol), lithium chloride (2.3 mg, 0.054 mmol), and copper(I) iodide (1.0 mg, 0.005 mmol) were taken in a microwave vial and the vial was vacuum pumped and flushed with argon three times. To this mixture was added 1-methyl-5-(4-(tributylstannyl)pyrimidin-2-yl)-1H-indazole (9.0 mg, 0.018 mmol) in degassed 1,4-dioxane (0.5 mL). The reaction mixture was heated at 100° C. for 5 h, 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 C33H31ClN5O3S: 612.2 (M+H+); Found: 611.9 (M+H+).

1. customflushed with argon three times
2. temperaturecooled
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