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Compound of butenafine hydrochloride, preparation method, and application as medication for restraining and killing fungus

A technology of butenafine hydrochloride and its compound, which is applied in the field of compound and its preparation, can solve the problems of single mechanism of action, decreased therapeutic effect, high recurrence rate of symptoms, etc., and achieve long action time, low drug resistance and low recurrence rate Effect

Inactive Publication Date: 2006-02-01
焦家良
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the skin topical drugs are basically imidazole antifungal drugs. The mechanism of action of this kind of products is single. They only affect the membrane permeability by interfering with ergosterol synthesis to inhibit fungal growth. Moreover, most products have been on the market for too long, and cross-resistance is common. , the recurrence rate of symptoms is high, and the treatment effect is reduced

Method used

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  • Compound of butenafine hydrochloride, preparation method, and application as medication for restraining and killing fungus
  • Compound of butenafine hydrochloride, preparation method, and application as medication for restraining and killing fungus
  • Compound of butenafine hydrochloride, preparation method, and application as medication for restraining and killing fungus

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Experimental program
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Effect test

Embodiment 1

[0027] Such as figure 1 As shown, N-methyl-1-naphthylmethylamine, p-tert-butylbenzyl chloride, anhydrous sodium carbonate, DMF (dimethylformamide) were purchased from the market, and 685g (4.0mol) N- Methyl-1-naphthylmethylamine, 730g (4.0mol) of p-tert-butylbenzyl chloride, 424g (4.0mol) of anhydrous sodium carbonate and 3000ml of DMF were successively put into the reaction flask, and stirred and reacted at 50-60°C for 16 hours. After cooling, pour the reaction mixture into an appropriate amount of ice water; add acid to make it strongly acidic, and precipitate a solid, cool, filter the solid, and recrystallize with ethanol-ethyl acetate to obtain 1100 g of a white solid product, which is the target compound cloth hydrochloride. For tenafine, the yield is 77.7%. The added acid can be selected from sulfuric acid, nitric acid or hydrochloric acid, and concentrated sulfuric acid is selected in this embodiment.

[0028] Prepare liniment according to the following prescription w...

Embodiment 2

[0034] 343g (2.0mol) of N-methyl-1-naphthylmethylamine, 365g (2.0mol) of p-tert-butylbenzyl chloride, 212g (2.0mol) of anhydrous sodium carbonate and 1500mlDMF were dropped into the reaction flask successively, at 50 The reaction was stirred at -60°C for 16 hours. After cooling, the reaction mixture was poured into ice water; nitric acid or hydrochloric acid was added to make it strongly acidic, and a solid was precipitated. Cool, collect the solid by filtration, and recrystallize with ethanol-ethyl acetate to obtain 550 g of a white solid product which is the target compound butenafine hydrochloride, with a yield of 77.7%.

[0035] Buy stearic acid, white petrolatum, glyceryl monostearate, polysorbate, propylene glycol, methyl cellulose, ethylparaben from the market, and use the prepared butenafine hydrochloride to prepare milk according to the following prescription Ointment (percentage by weight): 0.08-0.1% butenafine hydrochloride, 9-12% stearic acid, 7-10% white petrolat...

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Abstract

A compound, butenafine hydrochloride C23H27N?HCL, its preparing process and its application in preparing medicine for suppressing and killing funguses are disclosed. Its advantages are broad spectrum, quickly taking its high curative effect, and no recurrence.

Description

technical field [0001] The invention relates to a compound and its preparation method, and the technical field of using the compound to prepare drugs capable of inhibiting and killing fungi. Background technique [0002] my country is an area with a high incidence of fungal skin diseases, and there are 500 million patients of various types. The society needs more effective and safe antifungal skin topical drugs. At present, the skin topical drugs are basically imidazole antifungal drugs. The mechanism of action of this kind of products is single. They only affect the membrane permeability by interfering with ergosterol synthesis to inhibit fungal growth. Moreover, most products have been on the market for too long, and cross-resistance is common. , the recurrence rate of symptoms is high, and the treatment effect is reduced. At present, there is an urgent need for a new generation of antifungal drugs to serve patients. Contents of the invention [0003] In order to make ...

Claims

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Application Information

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IPC IPC(8): C07C211/27A61K31/137A61K9/06A61P31/10
Inventor 焦家良
Owner 焦家良
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