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Treatment method of bilastine reaction mother liquor

A bilastine and reaction technology, applied in the field of medicinal chemistry, can solve the problems of complex synthesis steps, long synthesis routes, expensive raw materials and catalysts, etc., and achieve the effects of simple operation, easy product, and improved overall reaction yield

Inactive Publication Date: 2014-04-30
万全万特制药江苏有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] At present, there are many synthesis routes for Bilastine, but most of them are relatively long, the synthesis steps are complex, and the raw materials and catalysts used are expensive

Method used

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  • Treatment method of bilastine reaction mother liquor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1: 2-(4-(2-(4-(1-(2-ethoxy-ethyl)-1H-benzimidazol-2-yl)-piperidin-1-yl)-ethyl )-phenyl)-2-methyl-propionic acid synthesis (preparation mother liquor recovery)

[0013] In a 500ml three-neck flask, add 40.2g of the residue obtained after the preparation mother liquor of bilastine was spin-dried, 300ml of acetic acid, and stirred at 60°C for 40h. After the reaction was completed, 2-(4-(2-(4-(1 -(2-Ethoxy-ethyl)-1H-benzimidazol-2-yl)-piperidin-1-yl)-ethyl)-phenyl)-2-methyl-propionic acid, yield 82 %.

[0014] 1 HNMR (CDCl 3 ):1.05-1.07(t 3H), 1.53(s 6H), 2.28(s 5H), 3.12-3.82(m 12H), 4.52(s 2H), 7.29-7.62(m 8H)

Embodiment 2

[0015] Example 2: 2-(4-(2-(4-(1-(2-ethoxy-ethyl)-1H-benzimidazol-2-yl)-piperidin-1-yl)-ethyl )-phenyl)-2-methyl-propionic acid synthesis (preparation mother liquor recovery)

[0016] In a 250ml three-neck flask, add 29.0g of the residue obtained after the preparation mother liquor of bilastine was spin-dried, add 150ml of 3N hydrochloric acid, and stir at 70°C for 20h. After the reaction is completed, 2-(4-(2-(4- (1-(2-Ethoxy-ethyl)-1H-benzimidazol-2-yl)-piperidin-1-yl)-ethyl)-phenyl)-2-methyl-propionic acid, yield The rate is 89%.

Embodiment 3

[0017] Example 3: 2-(4-(2-(4-(1-(2-ethoxy-ethyl)-1H-benzimidazol-2-yl)-piperidin-1-yl)-ethyl )-phenyl)-2-methyl-propionic acid synthesis (preparation mother liquor recovery)

[0018] Other conditions were constant, the solvent was changed to a mixed solution of 3N hydrochloric acid and acetic acid, and the yield was 79%.

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Abstract

The invention belongs to the field of pharmaceutical chemistry and relates to a treatment method of a bilastine reaction mother liquor. The treatment method is characterized in that the bilastine reaction mother liquor is dissolved in acid water after being spin-dried, and then stirred for 0-78 hours at a certain temperature, and finally, after-treatment refining is carried out to obtain the qualified product of bilastine, namely, a compound 1.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a method for recovering bilastine from a mother liquor prepared by a bilastine method. Background technique [0002] Bilastine, the chemical name is 2-(4-(2-(4-(1-(2-ethoxy-ethyl)-1H-benzimidazol-2-yl)-piperidine- 1-yl)-ethyl)-phenyl)-2-methyl-propionic acid, the second generation of histamine H developed by Faes Pharmaceutical Company of Spain 1 Receptor antagonists are mainly used clinically to treat allergic rhinitis and chronic idiopathic urticaria, and their structural formula is as follows: [0003] [0004] At present, there are many synthetic routes for bilastine, but most of them are relatively long, the synthetic steps are complex, and the raw materials and catalysts used are expensive. How to increase the reaction yield as much as possible and reduce energy consumption is of great significance both from an economic point of view and the green chemist...

Claims

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Application Information

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IPC IPC(8): C07D401/04
CPCC07D401/04
Inventor 靳旭霞闫起强马苏峰
Owner 万全万特制药江苏有限公司
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