Hydrochloric Acid → Hydrochloric Acid

Participants

Reaction Steps

4-(3-Chloro-4-cyano-phenylamino)-piperidine-1-carboxylic acid tert-butyl ester (290 mg; 0.87 mmol, prepared according to Example 103) is dissolved in dichloromethane (1.3 mL) and trifluoroacetic acid (0.7 mL) is added under stiffing. After 60 minutes, the reaction mixture is concentrated under reduced pressure and the residue obtained is co-evaporated with dichloromethane (2×5 mL). The product is then diluted in dioxane (1 mL) and a 4N solution of hydrochloric acid in dioxane (2 mL) is added. The precipitate formed is filtered and dried under high vacuum at 40° C. to afford the desired product as hydrochloride (210 mg; 0.77 mmol).

Provenance & Evidence