Novel preparation method of hydroxychloroquine sulfate

A technology of hydroxychloroquine sulfate and hydroxychloroquine, which is applied in the field of medicine and chemical industry, can solve the problems affecting the purification of hydroxychloroquine free base, high difficulty in operation, and difficult removal, so as to reduce production cost and pollution control cost, and the post-processing is simple and avoids The effect of impurity inclusion
CN109456266AInactive Publication Date: 2019-03-12南京天际联盟医药科技有限公司
10 Cites 13 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
南京天际联盟医药科技有限公司
Publication Date
2019-03-12
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses a preparation method of hydroxychloroquine sulfate. The preparation method is characterized in that a parent core 4,7-dichloroquinoline used as a starting material and a hydroxychloroquine side chain 5-(N-ethyl-N-2- ethanolamine)-2-amylamine undergo condensation reaction in the presence of a catalyst to obtain a hydroxychloroquine free base, and then the hydroxychloroquinefree base undergoes salt formation with sulfuric acid to obtain the hydroxychloroquine sulfate. The preparation method overcomes the disadvantages in the prior art, and has the advantages that the useamount of the side chain is reduced; the total yield is more than or equal to 90 percent; the yield of the hydroxychloroquine sulfate is more than or equal to 96 percent; the total yield is more thanor equal to 86 percent; the purity of the hydroxychloroquine sulfate is more than 99. 7 percent; and the single impurity is less than 0.1 percent. The preparation method meets the pharmacopoeia requirements and is short in reaction time, easy and convenient to operate, low in pollution, low in cost and suitable for industrial production.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the technical field of medicine and chemical industry, and specifically designs hydroxychloroquine sulfate, which is a medicine for treating discoid lupus erythematosus and systemic lupus erythematosus. Background technique

[0002] Hydroxychloroquine Sulfate (Hydroxychloroquine Sulfate, HCQ) chemical name is 2-[[4-[(7-chloro-4-quinolyl)amino]pentyl]ethylamino]-ethanol sulfate, CAS number is 747-36- 4. The chemical structure is as follows:

[0003]

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

[0005] US2546658 discloses a kind of synthetic method of hydroxychloroquine sulfate, and the reaction process of this ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More