反应详情

温度

110 °C

(S)-2-tert-butoxy-2-(7-(4-chlorophenyl)-2-(2-chloropyridin-4-yl)-5-methylbenzo[d]thiazol-6-yl)ethyl pivalate (19.7 mg, 0.034 mmol), 3-cyanophenylboronic acid (6.1 mg, 0.041 mmol), Pd(PPh3)4, and K2CO3 (14.3 mg, 0.103 mmol) were placed in a microwave vial and the vial was vacuum pumped and flushed with argon three times. To this mixture was added degassed 1,4-dioxane (0.4 mL) and degassed water (0.1 mL). The reaction mixture was heated at 110° C. for 1.5 h, cooled, diluted with ethyl acetate, 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 C37H37ClN3O3S: 638.2 (M+H+); Found: 637.9 (M+H+).

1. customflushed with argon three times
2. additionTo this mixture was added
3. customdegassed 1,4-dioxane (0.4 mL)
4. customdegassed water (0.1 mL)
5. temperaturecooled
6. additiondiluted with ethyl acetate
7. filtrationfiltered through Celite (ethyl acetate eluent)
8. concentrationconcentrated
9. customPurification by flash column chromatography on silica gel (hexanes/ethyl acetate eluent)
10. customprovided the product