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Flucytosine preparation method applicable to industrial production

A technology of flucytosine and fluoropyrimidine, which is applied in the field of pharmaceutical chemical synthesis, can solve the problems of complex production process, low purity and yield of flucytosine, and increased input cost, and achieve low input cost, good prospects, and simple operation Effect

Inactive Publication Date: 2017-01-25
宿迁市万和泰化工有限公司
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  • Summary
  • Abstract
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AI Technical Summary

Problems solved by technology

[0003] However, the existing production process of chlorocytosine is relatively complicated, and the purity and yield of fluorocytosine produced are relatively low, which increases input costs.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0022] A preparation method applicable to flucytosine for industrial production, the preparation method comprising the following steps:

[0023] (1) Chlorination process

[0024] Add fluorouracil and phosphorus oxychloride into the chlorination pot, stir, control the temperature below 15°C, low-priced N,N-dimethylaniline; after the dropwise addition, raise the temperature to about 110°C for 2 hours; cool to room temperature , placed in ice-salt water for ice-thawing, maintained at 15°C, and stirred for 1.5 hours; filtered and washed with water to obtain 2,4-dichloro-fluoropyrimidine;

[0025] (2) Ammonification process

[0026] Dissolve 2,4-dichloro-fluoropyrimidine in ethanol, stir, and add ammonia water dropwise at a temperature below 35°C. After dropping, cool down to 25°C and react for 3.5 hours, depressurize the culprit ethanol to dryness, add water and stir to raise the temperature to 20°C ; Filter, wash the crystals with water, and dry to obtain 4-amino-2-chloro-fluor...

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PUM

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Abstract

The invention discloses a flucytosine preparation method applicable to industrial production. The method comprises the following steps: performing chlorination on fluorouracil, performing ammonification, and performing hydrolysis, thereby obtaining flucytosine. To solve defects, the invention provides the flucytosine preparation method applicable to industrial production, and the method is small in process procedure, simple in operation, low in investment cost, relatively good in prospect and applicable to large-scale industrial production.

Description

technical field [0001] The invention relates to the technical field of medicinal chemical synthesis, in particular to a preparation method of flucytosine suitable for industrial production. Background technique [0002] Flucytosine is used to treat fungal infections caused by cryptococcus and candida, such as fungal sepsis, endocarditis, meningitis, and antifungal drugs for lung and urinary tract infections. It is mainly used for mucocutaneous candidiasis, candida endocarditis, candida arthritis, cryptococcal meningitis and coloring fungal disease. During the period of medication, the blood picture should be checked regularly. Patients with hepatic and renal insufficiency, blood diseases and pregnant women should be used with caution; patients with severe renal insufficiency are contraindicated. This product is used as the first choice drug for the treatment of severe systemic albicans and cryptococcal infection abroad, and is used for the treatment of fungal meningitis, f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/47
CPCC07D239/47
Inventor 张正荣张辉吴广磊
Owner 宿迁市万和泰化工有限公司
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