反应详情

To a mixture of tert-butyl 4-(4-(2-chloropyrimidin-4-yl)-1H-pyrazol-1-yl)-4-(cyanomethyl)piperidine-1-carboxylate (0.487 g, 1.21 mmol) in 2 mL of dioxane was added 4 M HCl in dioxane (4.0 mL). The reaction was stirred at room temperature for 30 min, then evaporated to dryness. To the resulting crude HCl salt in methylene chloride (9.4 mL) was added triethylamine (0.505 mL, 3.62 mmol) followed by cyclopropanesulfonyl chloride (0.148 mL, 1.45 mmol). The mixture was stirred at room temperature for 30 min, washed with saturated sodium bicarbonate, dried, and evaporated to dryness. The residue was used directly in next step (402 mg, 82%). LCMS (M+H) 407.0.

1. customevaporated to dryness
2. stirringThe mixture was stirred at room temperature for 30 min
3. washwashed with saturated sodium bicarbonate
4. customdried
5. customevaporated to dryness