Process for synthesizing 5-aminovaleric acid hydrochloride

A technology of amino ketovalerate hydrochloride and synthesis method, applied in chemical instruments and methods, preparation of organic compounds, organic chemistry and other directions, can solve the problems of low production cost, low yield, high price and the like, and achieves easy operation. , the raw materials are easily available, and the effect is conducive to industrial production
CN101462974AActive Publication Date: 2009-06-24FUJIAN BOTE CHEM PROD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
FUJIAN BOTE CHEM PROD
Publication Date
2009-06-24

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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.
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Description

Technical field:

[0001] The invention relates to the field of synthesis of medical compounds, in particular to a synthesis method of 5-aminolevulinic acid hydrochloride. Background technique:

[0002] Photodynamic therapy (PDT) was created in the 1970s. Due to the development and progress of photosensitive substances in recent years, 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.

[0003] Although the structure of 5-aminolevulinic acid hydrochloride is simple, its synthesis is quite difficult, especially the process for industrial production. The main synthetic methods can be summarized as:

[0004] 1. Using glycine as raw material, phthalic amidation, acyl chloride, condensation, decarboxylation, hydrolysis (J.Chem.Soc.(1954, 18...

Claims

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