Process for synthesizing 5-aminovaleric acid hydrochloride

Abstract

The invention relates to an efficient novel method for synthesizing photosensitizing agent 5-ketoamine valerate hydrochloride. The method uses compounds of formula (I) and formula (II). In the formulas, R1 and R2 represent hydrogen or C1-C4 alkyl or substituted benzyl; R3 represents the C1-C4 alkyl or the substituted benzyl; and X represents Cl, Br, OTs and OMs. High purity 5-ketoamine valerate hydrochloride is prepared after alkylation reaction, interesterification, hydroxylamination, reduction and hydrolysis decarboxylation finally. R1=H, alkyl or substituted benzyl group; X=Cl, Br, OTs, OMs; R2=H, alkyl or substituted benzyl group; R3=alkyl or substituted benzyl group.

Description

Technical field: The present invention relates to the synthetic field of medical compound, relate in particular to a kind of synthetic method of 5-aminolevulinic acid hydrochloride. Background technique: Photodynamic therapy (PDT) was pioneered in the 1970s. In recent years, due to the development and progress of photosensitive substances, etc., it has gradually become one of the basic methods for treating tumors. 5-aminolevulinic acid hydrochloride is the hydrochloride salt of a new generation of photodynamic therapy drug 5-aminolevulinic acid (5-ALA), which is clinically used for actinic keratosis (Actinic Keratoses, AK) Treatment. Although the structure of 5-aminolevulinic acid hydrochloride is simple, its synthesis is quite difficult, especially the technology that can carry out industrialized production. The main synthetic methods can be summarized as: 1. Using glycine as raw material, phthalic amidation, acyl chloride, condensation, decarboxylation, hydrolysis (J....

AI Technical Summary

Problems solved by technology

The technical problem to be solved by this invention is to provide a kind of synthetic method of 5-aminolevulinic acid hydrochloride, to solve the defects in the prior art