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Preparation method of epinastine impurity A

A technology of epinastine and impurity, which is applied in the field of preparation of epinastine impurity A, can solve the problems of epinastine impurity A, such as low purity, low reaction conversion rate, and many side reactions, and achieve simple process, The effect of high purity and convenient operation

Active Publication Date: 2021-04-16
广州艾格生物科技有限公司
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Problems solved by technology

[0006] In view of this, the application provides a preparation method of epinastine impurity A, which can effectively solve the problem of the existing epinastine impurity A preparation method with many side reactions or low reaction conversion rate resulting in the preparation of epinastine impurity A technical defect of low purity and low yield

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  • Preparation method of epinastine impurity A
  • Preparation method of epinastine impurity A
  • Preparation method of epinastine impurity A

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Embodiment

[0037] The embodiment of the present application provides a kind of epinastine impurity A, and its preparation method comprises:

[0038] Step 1: Add 7.9g of epinastine free base, 6.0g of Pd / C, 200mL of toluene into the reaction flask, heat to 110°C and reflux for 26h to prepare reactant 1.

[0039] Step 2: The reactant 1 in step 1 is filtered and washed in sequence to obtain a substance after removing Pd / C, which is then concentrated to obtain reactant 2.

[0040] Step 3: Add the reactant 2 of step 2 into acetone to make a slurry, filter and then vacuum-dry to obtain an off-white solid product.

[0041] The product of the embodiment of the present application is carried out HPLC spectrogram, proton nuclear magnetic spectrum spectrogram and mass spectrogram analysis, the result is as follows Figure 1 ~ Figure 3 shown. from Figure 1 ~ Figure 3 It can be seen that the product obtained in the examples of the present application is epinastine impurity A. The mass of epinasti...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of an epinastine impurity A. The invention provides a preparation method of an epinastine impurity A. The preparation method comprises the following steps: step 1, mixing epinastine free alkali, a hydrogenation catalyst and a reaction solvent, and carrying out heating reaction to prepare a reactant 1; step 2, filtering the reactant 1, removing the hydrogenation catalyst, and concentrating to obtain a reactant 2; and step 3, mixing the reactant 2 with a pulping solvent, pulping, filtering and drying to obtain an epinastine impurity A. The epinastine free alkali has a structure as shown in a formula I. The invention provides a preparation method of an epinastine impurity A. The technical defects of low purity and low yield of the prepared epinastine impurity A caused by many side reactions or low reaction conversion rate of an existing preparation method of the epinastine impurity A can be effectively overcome.

Description

technical field [0001] The application belongs to the technical field of medicine, in particular to a preparation method of epinastine impurity A. Background technique [0002] Epinastine hydrochloride (3-amino-9,13b-dihydro-1H-diphenyl[c,f]imidazo[1,5-a]azepine hydrochloride, ) is a histamine H1 receptor antagonist, which has inhibitory effects on histamine, leukotriene C4, PAF, and serotonin, and can also inhibit the release of histamine and slow-reacting substance A (SRS-A) chemical mediators. It can be used for the prevention and treatment of allergic rhinitis, urticaria, eczema, dermatitis, skin pruritus, pruritus, psoriasis vulgaris with pruritus 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 impurities: impurity A (3-amino-9H-diphenyl[c,f]imidazo[1,5-a]azepine, ...

Claims

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Application Information

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IPC IPC(8): C07D487/04
CPCY02P20/584
Inventor 尹科郑镇东张现涛何盛江谭斌
Owner 广州艾格生物科技有限公司
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