反応 #152

ord-dd820c31fef4456fb96fcbe0cfbfed80

反応方程式

Brc1ccc(CN2CCOCC2)cc1
Brc1ccc(CN2CCOCC2)cc
Cc1ncc(-c2nc(N)ncc2F)n1C1CCOCC1
Cc1ncc(-c2nc(N)ncc2F
Cc1ncc(-c2nc(Nc3ccc(CN4CCOCC4)cc3)ncc2F)n1C1CCOCC1
Cc1ncc(-c2nc(Nc3ccc(

反応条件

温度
100°CELSIUS

実験手順

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.

出典

750 AstraZeneca ELN dataset