反应 #112
ord-b9ea1ddb99074c47af3b567d6c34306c
反应方程式
Fc1cc(CN2CCOCC2)ccc1
Cc1ncc(-c2nc(N)ncc2F
→
Cc1ncc(-c2nc(Nc3ccc(
收率 88.0%
反应条件
温度
110°CELSIUS
实验过程
The aim of the reaction is test/optimization: 5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine (100 mg, 0.36 mmol), 4-(4-bromo-3-fluorobenzyl)morpholine (109 mg, 0.40 mmol), Palladium, 10% On Charcoal (115 mg, 0.11 mmol), Tri-o-tolylphosphine (49.4 mg, 0.16 mmol) and Sodium tert-pentoxide (79 mg, 0.72 mmol) were dissolved in toluene (1.5 mL) and heated to 110 °C under argon. The reaction was monitorred by HPLC. After 16 h 88 % conversion was achieved. The reaction was stopped and the mixture was discarded.
来源
750 AstraZeneca ELN dataset