Preparation method of bilastine

A technology of bilastine and molar ratio, which is applied in the field of preparation of the compound of formula I of bilastine raw material medicine, and can solve the problem of generating quaternary ammonium salt by-products and the like
CN110950837APending Publication Date: 2020-04-03上海天慈中商药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
上海天慈中商药业有限公司
Publication Date
2020-04-03

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Abstract

The invention provides a preparation method of bilastine. Specifically the method comprises the following steps: oxidizing 4-hydroxyethyl phenyl methyl tert-butyrate to obtain 4-acetaldehyde phenyl methyl tert-butyrate, and carrying out a reductive amination reaction on the 4-acetaldehyde phenyl methyl tert-butyrate and a compound represented by a formula IV to obtain 4-[2-[1-(2-ethoxyethyl)benzimidazolyl]piperidyl]ethyl-phenyl methyl tert-butyrate (represented by a formula V); and hydrolyzing and acidifying the compound represented by the formula V to obtain bilastine. The method is high in yield, simple to operate and suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of a bilastine raw material compound of formula I. Background technique

[0002] Bilastine is the second generation of histamine H developed by Spanish FAES pharmaceutical company 1 Receptor antagonist is a non-sedating long-acting antihistamine that selectively antagonizes peripheral H1 receptors, has no affinity for muscarinic receptors, and has low affinity for other receptors. For the treatment of allergic rhinoconjunctivitis (seasonal and perennial) and urticarial diseases. This product is safe, without the cardiotoxicity and sedative effects of commonly used antihistamines.

[0003] Patents ES2151442A1, CN104402773A, Kong Hao, etc. (Chinese Journal of Pharmaceutical Industry, 2015, 46 (7)) reported the synthesis method of bilastine:

[0004]

[0005] The alkylation reaction of this method needs to use inflammable and explosive sodium...

Claims

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