Hydroxychloroquine sulfate and preparation method thereof

A technology of hydroxychloroquine sulfate and hydroxychloroquine, applied in the field of chemistry or medicinal chemistry, can solve the problems of long production time, cumbersome process, unfriendly environment, etc., and achieve the effects of reducing pollution and consumption, avoiding high pollution, and simple and rapid operation.
CN113185459APending Publication Date: 2021-07-30JIANGXI GUOYAO PHARMA LLC +1
3 Cites 2 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JIANGXI GUOYAO PHARMA LLC
Publication Date
2021-07-30

Smart Images

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

Abstract

The invention discloses hydroxychloroquine sulfate and a preparation method thereof, and relates to the technical field of medicinal chemistry. The preparation method comprises the steps of mixing 4, 7-dichloroquinoline with a hydroxychloroquine side chain, carrying out heating condensation in the presence of an organic base catalyst, adding water and liquid, and carrying out cooling crystallization to obtain hydroxychloroquine; and dissolving hydroxychloroquine in an ethyl acetate and ethanol aqueous solution, heating, dissolving and clarifying, dropwise adding concentrated sulfuric acid, cooling, crystallizing, filtering and drying to obtain hydroxychloroquine sulfate. The method has the beneficial effects that a solvent-free reaction is used, and a catalyst is added, so that high pollution is avoided, the reaction process is accelerated, and the operation is simple; and meanwhile, the HPLC purity of the obtained hydroxychloroquine refined product is not less than 96.50%, the maximum single impurity content is less than 0.10%, the yield can reach 85%, the HPLC purity of hydroxychloroquine sulfate is not less than 98.00%, the maximum single impurity content is less than 0.10%, and the yield can reach 90%.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the field of chemistry or medicinal chemistry, and in particular relates to a hydroxychloroquine sulfate and an industrial preparation method thereof. Background technique

[0002] Hydroxychloroquine Sulfate (Hydroxychloroquine Sulfate), its chemical name is 2-[[4-[(7-chloro-4-quinolyl)amino]pentyl]ethylamino]-ethanol sulfate. Successfully developed by Winthrop Company, it was first listed in the United States in 1956, and has been 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.

[0003] U.S. Patent US2546658A discloses a kind of synthetic method of hydroxychloroquine sulfate, and this method is reported in 1951, and this patent adopts 4,7-dichloroquinoline and 5-(N-ethyl-N-2-hydroxyethylenediylamino)- 2-pentylamine (hereinafter referred to as hydroxychloro...

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