PROCESS FOR THE PREPARATION OF COLESEVELAM

摘要

The present invention relates to a new process for the synthesis of Colesevelam, which is used in therapy in cases of hypercholesterolemia due to low density lipoproteins. Said process comprises the reaction, in a basic environment, of polyallylamine with: i) at least one alkylating agent of formula X—(CH2)9—CH3 and at least one alkylating agent of formula Y—(CH2)6—N+ (CH3)3Z−, wherein X and Y are each independently a leaving group, and Z is a halogen; and ii) at least one crosslinking agent. The present invention also relates to the Colesevelam obtainable by the above process.

主权项

1. Process for the synthesis of Colesevelam comprising reacting, in a basic environment, polyallylamine with:
i) at least one alkylating agent of formula X—(CH2)9—CH3 and at least one alkylating agent of formula Y—(CH2)6—N+(CH3)3Z−, wherein X and Y are each independently a leaving group, and Z is a halogen; and ii) at least one crosslinking agent, wherein said at least one alkylating agent of formula X—(CH2)9—CH3, said at least one alkylating agent of formula Y—(CH2)6—N+(CH3)3Z−, and said at least one crosslinking agent are reacted with polyallylamine simultaneously.