A kind of industrialized preparation method of hydroxychloroquine sulfate

A technology of hydroxychloroquine sulfate and hydroxychloroquine sulfate, which is applied in the field of preparation of hydroxychloroquine sulfate, can solve problems such as unfavorable recycling and environmental protection, increase production costs, and cumbersome production processes, so as to save extraction agent and labor costs, and save production Cost, the effect of reducing environmental pollution
CN103724261BActive Publication Date: 2016-05-25WUHAN WUYAO PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
WUHAN WUYAO PHARMA
Publication Date
2016-05-25

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Abstract

The invention provides an industrial production method for hydroxychloroquine sulfate, which includes the following steps: enabling 4.7-dichloroquinoxaline and 5-(N-ethyl-N-ethoxyl)-2-amino pentane to react under gas shield for 13-24 h at a gradually increased temperature of 120-130 DEG C to obtain hydroxychloroquine; preparing the hydroxychloroquine sulfate after the reaction between the hydroxychloroquine and an alcohol sulfate solution at the temperature of 20-30 DEG C. According to the method, the yield of the obtained crude product of the hydroxychloroquine is not smaller than 85%, the yield of the obtained hydroxychloroquine sulfate is not smaller than 85%, the yield of the obtained hydroxychloroquine sulfate HPLC is not smaller than 99.5%, the yield of single impurity is not larger than 0.1%, so that requirements of United States Pharmacopeia is met; the novel method is simple in procedure, is environment-friendly and easy in industrial production.
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Description

technical field

[0001] The invention relates to the field of medicinal chemistry, in particular to the preparation of hydroxychloroquine sulfate for treating discoid lupus erythematosus and systemic lupus erythematosus. Background technique

[0002] The chemical name of hydroxychloroquine sulfate is 2-[[4-[(7-chloro-4-quinolyl)amino]pentyl]ethylamino]-ethanol sulfate, and its chemical structure is as follows:

[0003]

[0004] Hydroxychloroquine sulfate was successfully developed by Winthrop Company and was first listed in the United States in 1956. It has been listed in France, Denmark, Japan, Germany, Finland and other countries and regions. The U.S. FDA approved Chlorine Sulfate Tablets on May 29, 1998 for the treatment of lupus erythematosus and rheumatoid arthritis.

[0005] US2546658 discloses a kind of hydroxychloroquine sulfate synthetic method, and the reaction process of this method is as follows:

[0006]

[0007] This patent was reported in 1951, and the ...

Claims

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