Formaldehyde → 3-(3,4-Difluorophenyl)-1-methylpyrrolidin-3-ol

Participants

Reaction Steps

Preparation according to Example 26: 3-(3,4-difluorophenyl)-pyrrolidin-3-ol (1.32 g, 6.63 mmol), formic acid (19.2 mL), aqueous formaldehyde (40%, 17.2 mL). 60° C. for 24 h. Yield: 0.83 g. The amine was converted to the fumaric acid salt and recrystallized from methanol/diethyl ether/diisopropyl ether: M.p. 164-166° C.; MS m/z (relative intensity, 70 eV) 213 (M+, 7), 141 (10), 113 (10), 58 (43), 57 (bp).

Provenance & Evidence