反応 #111

反応方程式

Fc1cc(CN2CCOCC2)ccc1

Cc1ncc(-c2nc(N)ncc2F

→

Cc1ncc(-c2nc(Nc3ccc(

収率 81.0%

溶媒

Cc1ccccc1

反応条件

実験手順

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), racemic-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (101 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 81 % conversion was achieved. The reaction was stopped and the mixture was discarded.

出典