Preparation method of voriconazole

A technology of voriconazole and methanol solution is applied in the field of pharmaceutical preparation, which can solve the problems of complex preparation process and high production cost, and achieve the effects of simple preparation method and low production cost

Inactive Publication Date: 2015-07-01
李磊
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Problems solved by technology

Because currently in the process of producing voriconazole, the preparation process is complicated and the production cost is high

Method used

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Embodiment Construction

[0006] Now in conjunction with the present invention for further detailed description.

[0007] A kind of preparation method of voriconazole of the present invention, concrete steps are as follows: at 0 ℃, in the methanol solution of sodium methoxide, add the methanol solution of ethyl α-fluoropropionyl acetate and formamidine acetate, cyclization obtains 6- Ethyl-5-fluoropyrimidin-4(3H)-one, it is refluxed with phosphorus oxychloride, chlorinated to obtain 4-chloro-6-ethyl-5-fluoropyrimidine, which is dissolved in tetrahydrofuran, in At -70°C, dropwise add lithium diisopropylamide in tetrahydrofuran solution, stir for 3 hours, add 1-(2,4-difluorophenyl)-2-(1H-1,2,4-tri Azol-1-yl) tetrahydrofuran solution of ethanone, the reaction gives 3-(4-chloro-5-fluoropyrimidin-6-yl)-2-(2,4-difluorophenyl)-1-(1H-1 , 2,4-triazol-1-yl)butan-2-ol, dissolved in ethanol, added 10% palladium-carbon and sodium acetate, hydrodechlorination, and then resolved to voriconazole.

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Abstract

The invention relates to a preparation method of voriconazole, wherein the preparation method comprises the following specific steps: adding alpha-fluoropropionyl ethyl acetate and a methanol solution of formamidine acetate into a methanol solution of sodium methylate, carrying out cyclization to obtain 6-ethyl-5-fluoropyrimidine-4(3H)-one, chloridizing to obtain 4-chloro-6-ethyl-5-fluoropyrimidine, dissolving 4-chloro-6-ethyl-5-fluoropyrimidine in tetrahydrofuran, dropwise adding into a tetrahydrofuran solution of lithium diisopropylamide, adding a tetrahydrofuran solution of 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazole-1-yl)ethyl ketone, carrying out a reaction to obtain 3-(4-chloro-5-fluoropyrimidine-6-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazole-1-yl)butyl-2-ol, dissolving in ethanol, adding 10% palladium-carbon and sodium acetate, and then splitting to obtain voriconazole. According to the preparation method of voriconazole, the preparation method is simple, and the production cost is low.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a preparation method of voriconazole. Background technique [0002] Voriconazole inhibits the demethylation of 14α-sterol mediated by cytochrome P450 in fungi, thereby inhibiting the biosynthesis of ergosterol. In vitro tests have shown that voriconazole has a broad-spectrum antifungal effect. Because currently in the process of producing voriconazole, the preparation process is complicated and the production cost is high. Contents of the invention [0003] The technical problem to be solved by the present invention is: in order to overcome the above-mentioned problems, a preparation method of voriconazole is provided. [0004] The technical scheme adopted by the present invention to solve the technical problem is: a preparation method of voriconazole, the specific steps are as follows: at 0°C, add ethyl α-fluoropropionyl acetate and formamidine acetic acid to the methanol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/06
CPCC07D403/06
Inventor 李磊
Owner 李磊
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