Malonic Acid → 3-Amino-3-(3,4-difluorophenyl)propanoic acid

Participants

Reaction Steps

697 g of 3,4-difluorobenzaldehyde (4.76 mol, 1 equivalent) were stirred together with 495 g of malonic acid (4.76 mol, 1 equivalent) and 733 g of ammonium acetate (9.52 mol, 2 equivalents) in 2788 ml of ethanol at reflux under argon for 20 h. Then the mixture was cooled to RT and stirred at RT overnight. The precipitated crystals were filtered off with suction, washed with ethanol and diethyl ether, and dried under reduced pressure. 590 g (62% of theory) of rac-3-amino-3-(3,4-difluorophenyl)propanoic acid were obtained.

Provenance & Evidence