反应详情

To a solution of 20% phosgene in toluene (phosgene:toluene=1:4, 54.9 uL, 0.104 mmol) was added a solution of 3-chloro-2-fluoroaniline (6.5 mg, 0.045 mmol) (Aldrich, Cat. #530174) and triethylamine (19.3 uL, 0.138 mmol) in THF (0.4 mL). The resulting mixture was stirred at r.t. for 2 h., and concentrated. To the residue was added a solution of 4-(4-methylpiperazin-1-yl)-6-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrimidin-2-amine HCl salt (15 mg, 0.034 mmol) and triethylamine (19.3 uL, 0.138 mmol) in acetonitrile (0.4 mL). The reaction mixture was stirred at r.t. for 30 min The mixture was purified by RP-LCMS (pH=10) to afford the desired product. Analytic LCMS (M+H)+: m/z=496.1/498.1.

1. concentrationconcentrated
2. stirringThe reaction mixture was stirred at r.t. for 30 min The mixture
3. customwas purified by RP-LCMS (pH=10)