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Method for preparing bepotastine besilate key intermediate

A technology of chlorophenyl and formate, which is applied in the field of preparing key intermediates of bepotastine besylate, which can solve the problems of unfavorable large-scale scale-up production and difficulty in convenient operation

Inactive Publication Date: 2018-07-20
WISDOM PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since this route involves the use of concentrated sulfuric acid, it is difficult to operate conveniently during mass production, and due to the strong acidity of concentrated sulfuric acid, the dehydration reaction of N-ethoxycarbonyl-4-piperidinol will also occur in the etherification process to produce ring Hexene impurities, so it is also unfavorable for large-scale scale-up production

Method used

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  • Method for preparing bepotastine besilate key intermediate
  • Method for preparing bepotastine besilate key intermediate
  • Method for preparing bepotastine besilate key intermediate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0026] 1, preparation formula III (R=Et) compound

[0027] Add compound formula II (X=Cl, R=Et) (200g, 910.5mmol) into a 10L four-necked flask, then add anhydrous toluene (3L), stir well and add NaI (1.36g, 9.1mmol) to the system, then A solution of compound formula I (185 g, 965 mmol) in anhydrous toluene (2 L) was added to the reaction system. After the addition, the system was heated to reflux for 6 hours, and after the reaction, the system was naturally cooled to room temperature. Toluene was distilled off under reduced pressure, and then CH was added to the system 2 Cl 2 (2.5L), add H to the system after stirring 2 O (1L), stirred for 10 minutes, then the system stood still, and the organic phase was separated. CH for aqueous phase 2 Cl 2 (2 x 300 mL) and combine the organic phases. The organic phase was washed with 2% saturated aqueous sodium bicarbonate (300 mL), dried over anhydrous sodium sulfate, filtered, and the organic phase was distilled off under reduced ...

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Abstract

The invention relates to a method for preparing a bepotastine besilate key intermediate, in particular to 4-[(4-chlorphenyl)(2-pyridyl)methoxyl]piperidine-1-formate prepared from alpha-(4-chlorphenyl)-2-pyridinemethanol and 4-halogenated piperidine-1-carboxylate through a reaction.

Description

technical field [0001] The invention relates to the field of chemical synthesis, in particular to a method for preparing a key intermediate of bepotastine besylate. Background technique [0002] Bepotastine besylate is a histamine H1 receptor antagonist jointly developed by Japan UBE Company and Japan Tanabe Seiyaku Company. This drug is a non-sedative highly selective histamine receptor antagonist and has a stabilizing effect on mast cells , can prevent eosinophils from migrating to inflammatory tissues and can inhibit interleukin-5 (IL-5), leukotriene B4 (LTB4) and platelet activating factor (PAF), and reduce allergic inflammation. A variety of in vivo and in vitro animal tests have shown that bepotastine besilate has significant antihistamine / allergy effects and can improve allergic conjunctival inflammation in animals. The drug is clinically used to treat allergic rhinitis, conjunctivitis, skin reactions, etc., and has obvious effects on sneezing, itching, nasal congest...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07C57/15C07C51/41
CPCC07D401/12
Inventor 邹平邱小龙胡林储玲玲王平张程亮曾祥军吴忠平沈伟黄鑫许明张新刚时光好陈俊曹雷
Owner WISDOM PHARM CO LTD
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