4-(4-Bromobenzyl)morpholine → 5-fluoro-4-[2-methyl-3-(oxan-4-yl)imidazol-4-yl]-N-[4-(morpholin-4-ylmethyl)phenyl]pyrimidin-2-amine

関与物質

反応条件

反応手順

Tris(dibenzylideneacetone)dipalladium(0) (4.5 mg, 4.91 µmol) and 2-Dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (4.38 mg, 9.20 µmol) were dissolved in butyl acetate (1.8 mL) in a 10 mL Schlenk tube and activated at 100 °C for 6 min under argon. Then 5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine (51 mg, 0.18 mmol), 4-(4-bromobenzyl)morpholine (49.5 mg, 0.19 mmol) and Sodium tert-pentoxide (32.4 mg, 0.29 mmol) were added. It was degassed again and stirred at 100 °C under argon. The reaction was followed by HPLC. After 4.5 h no conversion was observed. Hence the whole reaction mixture was discarded.

情報源と証拠