反应 #113

ord-572b233d6c664fada44bd8d3bb48fc2f

反应方程式

Fc1cc(CN2CCOCC2)ccc1Br
Fc1cc(CN2CCOCC2)ccc1
Cc1ncc(-c2nc(N)ncc2F)n1C1CCOCC1
Cc1ncc(-c2nc(N)ncc2F
Cc1ncc(-c2nc(Nc3ccc(CN4CCOCC4)cc3F)ncc2F)n1C1CCOCC1
Cc1ncc(-c2nc(Nc3ccc(
收率 73.0%

溶剂

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), Triphenylphosphine (0.038 mL, 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 73 % conversion was achieved. The reaction was stopped and the mixture was discarded.

来源

750 AstraZeneca ELN dataset