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Method for preparing butenafine hydrochloride

A technology of butenafine hydrochloride and acid-binding agent, which is applied in the field of medicine, can solve problems such as environmental pollution, and achieve the effects of reducing environmental pollution, reducing costs, and high yield

Inactive Publication Date: 2007-11-28
凌沛学
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0015] The purpose of the present invention is to provide a method for preparing butenafine hydrochloride with simple process, high yield and little environmental pollution, so as to solve the problems of environmental pollution, yield and production cycle of the existing preparation method

Method used

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  • Method for preparing butenafine hydrochloride
  • Method for preparing butenafine hydrochloride
  • Method for preparing butenafine hydrochloride

Examples

Experimental program
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Embodiment

[0024] Take 77g of N-methyl-1-naphthylmethylamine, 60g of polyethylene glycol-600, and 200ml of 5N NaOH solution, heat it to 95°C, slowly add 82g of p-tert-butylbenzyl chloride dropwise, and keep it warm for 3h. Cool down, add 300ml of chloroform to extract, wash with water 3 times, add 150ml of 6N HCl, measure pH to be about 2, separate to remove hydrochloric acid, wash with water until neutral, evaporate chloroform, add 300ml of ethyl acetate to reflux, filter, and recrystallize from ethanol-acetone to obtain 134g Product, yield 86.5%, MP: 211~215°C.

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Abstract

The present invention provides process of preparing Butenafine hydrochloride. Under the catalysis of phase transfer catalyst and in water as the reaction solvent, p-tert-butyl benzyl chloride and N-methyl-1-naphthyl methylamine react to produce Butenafine hydrochloride. The preparation process is simple, uses no toxic organic solvent, and has less environmental pollution, lowered cost, raised yield and shortened production period.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a preparation method of butenafine hydrochloride. Background technique [0002] Butenafine hydrochloride belongs to the third-generation allylamine antifungal drug, which has unique dual functions of inhibiting fungi and killing fungi. It can inhibit the activity of fungal squalene epoxidase at a lower concentration, causing fungal Insufficient squalene accumulation and ergosterol synthesis in the body: (1) squalene has a direct toxic effect on fungal cells, can cause rapid fungal death, and exhibits bactericidal activity; (2) ergosterol is necessary for the formation of fungal cell membranes Components whose insufficient synthesis inhibits fungal growth. [0003] Compared with traditional polyene and azole antifungal drugs, butenafine hydrochloride has the advantages of strong curative effect, less side effects and less recurrence, and has a greater market demand. [0004] There are three...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/27A61K31/137B01J31/06A61P31/10
Inventor 凌沛学王淑华贺艳丽刘爱华张玲汤漩
Owner 凌沛学
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