反应详情

4-(4-Trifluoromethoxy-phenylamino)-piperidine-1-carboxylic acid tert-butyl ester (380 mg; 1.06 mmol, prepared in accordance with Example 52) is dissolved in a 1 to 1 mixture of dichloromethane and trifluoroacetic acid (2 mL), and stirred for 90 minutes. The mixture is concentrated under reduced pressure and co-evaporated with dichloromethane (2×10 mL). The resulting residue is diluted in ethylacetate (5 mL) and a 4N solution of hydrochloric acid in dioxane (5 mL) is added. A precipitate is obtained which is filtered and dried under high vacuum to afford the desired product as hydrochloride (275 mg; 0.93 mmol).

1. concentrationThe mixture is concentrated under reduced pressure and co-evaporated with dichloromethane (2×10 mL)
2. additionThe resulting residue is diluted in ethylacetate (5 mL)
3. additiona 4N solution of hydrochloric acid in dioxane (5 mL) is added
4. customA precipitate is obtained which
5. filtrationis filtered
6. customdried under high vacuum