5-氟-2-(羟甲基)苯硼酸

反应条件: temp:100.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 10.405 g of (2-amino-6-iodoquinazolin-4-yl)-(1,3-dihydroisoindol-2-yl)methanone are dissolved in 450 ml of ethanol. 5 g of 5-fluoro-2-hydroxymethylphenylboronic acid, 10.4 g of potassium carbonate, 1 g of [1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloride and 450 μl of water are added to this solution, and the mixture is heated at 100° C. under argon for 1 h. The hot mixture is filtered off through Celite, and the filter cake is rinsed with 500 ml of hot ethanol. The filtrate is evaporated to dryness in vacuo, and the reddish residue obtained is triturated with 50 ml of acetonitrile, during which a beige solid precipitates out. This is filtered, washed with 20 ml of acetonitrile and dried at 40° C. in a drying cabinet for 16 h The hot mixture is filtered off through Celite the filter cake is rinsed with 500 ml of hot ethanol The filtrate is evaporated to dryness in vacuo the reddish residue obtained is triturated with 50 ml of acetonitrile, during which a beige solid precipitates out This is filtered washed with 20 ml of acetonitrile dried at 40° C. in a drying cabinet for 16 h