反应详情

温度

80 °C

A mixture of 1-[6-bromo-4-oxo-3-(2-trimethylsilanyl-ethoxymethyl)-3,4-dihydro-quinazolin-2-yl]-1H-pyrazole-4-carboxylic acid ethyl ester (0.500 g, 1.01 mmol), cyclopropylboronic acid (0.199 g, 2.32 mmol), dichloro(1,1′-bis(diphenylphosphino)ferrocene)palladium(II)dichloromethane adduct (0.100 g, 0.123 mmol), K2CO3 (0.420 g, 3.04 mmol) and THF (10 mL) were purged for 15 minutes with nitrogen and then heated to 80° C. for 15 h. The mixture was cooled to room temperature and filtered through a pad of CELITE®. The filtrate cake was washed with dichloromethane and concentrated. The residue was purified by FCC (0-20% EtOAc/hexanes) to yield the titled compound (0.120 g, 26% yield). MS (ESI/Cl): mass calcd. for C23H30N4O4Si, 454.2; m/z found, 455.2 [M+H]+.

1. customwere purged for 15 minutes with nitrogen
2. temperatureThe mixture was cooled to room temperature
3. filtrationfiltered through a pad of CELITE®
4. washThe filtrate cake was washed with dichloromethane
5. concentrationconcentrated
6. customThe residue was purified by FCC (0-20% EtOAc/hexanes)