Réaction #155

ord-bd19c64fd71c4dc0a1f39c0c85d4d230

Équation de réaction

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(

Solvants

Conditions de réaction

Température
90°CELSIUS

Mode opératoire

The aim of the reaction is only optimization and test. The reaction described below was carried out under argon atmosphere. Palladium(II) acetate (2.245 mg, 10.00 µmol) and (R)-(-)-1-[(S)-2-(Dicyclohexylphosphino)ferrocenyl]ethyldi-t-butylphosphine (5.61 mg, 10.00 µmol) were mixed in DME (0.2 mL) in a 1.4 ml vial under argon and stirred for 1 minute at room temperature. The orange pre-mixed Pd-catalyst solution were added to a 10 mL Schlenk-tube containing 4-(4-bromobenzyl)morpholine (0.282 g, 1.1 mmol) and Sodium tert- pentoxide (0.161 g, 1.46 mmol) in DME (1.5 mL). Finally, 5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine (0.277 g, 1 mmol) was added and the bright orange reaction mixture was stirred at 90 °C. The mixture turned from bright orange into bright yellow in 1 h. The reaction was followed by HPLC. No reaction took place, hence the mixture was discarded.

Source

750 AstraZeneca ELN dataset