反应详情

95 mg (0.32 mmol) of (R)-3-[(5-bromo-2-chloropyrimidin-4-yl)amino]-2-methyl-butan-2-ol is dissolved in 2 ml of acetonitrile and mixed with 116 mg (0.32 mmol) of (RS)—S-(4-aminophenyl)-S-cyclopropyl-N-[2-(trimethylsilyl)ethylsulfonyl]sulfoximide. After 0.08 ml of an approximately 4N solution of HCl in dioxane and 0.08 ml of water are added, the mixture is heated in a sealed vessel for 16 hours to 75° C. The suspension is filtered, and the filtrate is separated by flash chromatography (dichloromethane—dichloromethane/ethanol 95:5, 15 ml/min) The fractions, 43-51 min, contain 50 mg (25% of theory) of the desired product.

1. temperaturethe mixture is heated in a sealed vessel for 16 hours to 75° C
2. filtrationThe suspension is filtered
3. customthe filtrate is separated by flash chromatography (dichloromethane—dichloromethane/ethanol 95:5, 15 ml/min) The fractions, 43-51 min