Hydrochloric Acid → Melphalan hydrochloride

Participants

Reaction Steps

4-[Bis(2-chloroethyl)-amino]-L-phenylalanine (V) obtained in Example 2 was treated with concentrated hydrochloric acid (80 ml) at 25° C. to 30° C. and stirred at the same temperature for 15-20 hours. Toluene (1060 ml) was added and the resulting mixture was concentrated under reduced pressure till the moisture content of the residue was about 5%. Isopropyl alcohol (765 ml) was added to the resulting residue and stirred at 0° C. to 5° C. for 2-4 hours. 4-[Bis(2-chloroethyl)-amino]-L-phenylalanine hydrochloride thus obtained was filtered, washed with isopropyl alcohol (340 ml) and dried under reduced pressure at 45° C. to 50° C.

Provenance & Evidence