Malonic Acid → FTY720 Malonate

Participants

Reaction Steps

In an alternative procedure, FTY720 free base (2.27 mmol) was dissolved in ethyl acetate (16 ml) at 88 to 90° C. Then a solution of malonic acid (1.14 mmol) in ethyl acetate (3 ml) was added at 75° C., whereupon the product started to crystallize out immediately after addition. The resulting suspension was cooled to room temperature. The product was collected by filtration and was washed with ethyl acetate (2 ml). After drying at 50° C. the product (788 mg) was obtained as white crystals.

Provenance & Evidence