A kind of preparation method of epinastine related substance

A technology for epilastine and related substances, applied in the direction of organic chemistry and the like, can solve the problems of long reaction time, complicated process, low purity epilastine solution and the like, and achieves a simple preparation process, low cost and high yield. Effect
CN108997349BActive Publication Date: 2021-03-16HEFEI HUAFANG PHARMA SCI & TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HEFEI HUAFANG PHARMA SCI & TECH
Publication Date
2021-03-16

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Abstract

The invention discloses a preparation method of an epinastine related substance and relates to the technical field of medicines. The preparation method comprises steps as follows: epinastine is takenas a raw material, an oxidizing agent, a catalyst and a reaction system solvent are added, the mixture is stirred uniformly, an organic solvent is added after the reaction ends, extraction, washing, drying and suction filtration under reduced pressure are sequentially performed, and the organic solvent is recovered. An epinastine impurity A with the purity up to 97% is obtained through oxidation preparation, separation and purification steps, and the method is simple in preparation process, low in cost and high in yield.
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Description

technical field

[0001] The invention belongs to the technical field of medicine, in particular to a 3-amino-9H-diphenyl[c,f]imidazo[1,5-a]azepine (Epinastine impurity A) preparation method. Background technique

[0002] Epinastine hydrochloride (3-amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine Hydrochloride, formula 1) is a histamine H1 receptor antagonist, which has inhibitory effects on histamine, leukotriene C4, PAF, and serotonin, and can also inhibit histamine, slow-reacting substance A (SRS-A) The release of chemical mediators can be clinically used for the prevention and treatment of allergic rhinitis, urticaria, eczema, dermatitis, skin pruritus, prurigo, psoriasis vulgaris accompanied by itching, and allergic bronchial asthma. Common adverse reactions are allergies, drowsiness, digestive system symptoms and abnormal liver function.

[0003] The standard of epinastine hydrochloride included in European Pharmacopoeia version 8.7 contains two known impur...

Claims

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