Hydrochloric Acid → HCID 3080936, compound

Participants

Reaction Steps

450 mg of the polymer mainly comprising sodium of L-glutamate/L-alanine copolymer obtained in Example 3 was dissolved in 10 ml of water, to which an aqueous solution prepared by dissolving 66.3 mg of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC, condensing agent) in 5 ml of water was added. An aqueous solution prepared by dissolving 88.5 mg of P-[bis(2-chloroethyl)amino]L-phenylalanine (melphalan), which is a publicly known anti-cancer drug, in 20 ml of water was added dropwise to the mixed solution in 10 minutes. This reaction solution was stirred overnight at room temperature. When hydrochloric acid was added to the reaction solution to adjust the pH to 4.0, a white precipitate appeared. The precipitate was isolated by centrifugation and was washed with dilute hydrochloric acid. Thus obtained white solid was dissolved in 20 ml of 0.1 N caustic soda solution and dialyzed against pure water at 4° C. for 3 days on a permeable cellophane tube. The dialyzate was lyophilized to give 484 mg of L-glutamic acid/L-alanine copolymer sodium salt-melphalan conjugate as a curdy solid.

Provenance & Evidence