反应详情

75 mg of (2-amino-6-iodoquinazolin-4-yl)isoindolin-2-ylmethanone are suspended in 2 ml of tetrahydrofuran and 7 μl of water together with 40 mg of potassium 1-methyl-4-trifluoroboratomethylpiperazine, 1 mg of palladium diacetate, 4 mg of ((2,4,6 triisopropyl)phenyl)dicyclohexylphosphine and 176 mg of caesium carbonate, and the mixture is stirred at 80° C. for 48 h. After cooling, the mixture is filtered through kieselguhr, rinsed three times with 5 ml of tetrahydrofuran each time, and the filtrate is evaporated to dry ness in vacuo. The residue is purified by means of preparative HPLC, and the title compound is isolated.

1. temperatureAfter cooling
2. filtrationthe mixture is filtered through kieselguhr
3. washrinsed three times with 5 ml of tetrahydrofuran each time
4. customthe filtrate is evaporated
5. customto dry ness in vacuo
6. customThe residue is purified by means of preparative HPLC