A kind of preparation method of 5-fluorocytosine

A technology of flucytosine and fluoroacetonitrile, which is applied in the field of pharmaceutical chemical synthesis, can solve the problems of increased production cost and low reaction yield, and achieve the effects of prolonging service life, high purity, and improving atom utilization
CN110105290BActive Publication Date: 2020-06-23浙江伟锋药业有限公司
8 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
浙江伟锋药业有限公司
Publication Date
2020-06-23

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention provides a preparation method of 5-fluorocytosine. The method is characterized by including the following steps that 1, an organic solvent, fluoroacetonitrile, ethyl formate and organicbase are added into an autoclave for a heating reaction in a predetermined gaseous environment, then decompressing and cooling are conducted, and first reaction liquid containing an intermediate 1 isobtained; 2, an alcohol solution of hydrogen chloride is added into a reaction still, the first reaction liquid is added for reaction after cooling, a second reaction liquid is obtained after reaction, water is added into the second reaction liquid, the pH value is adjusted to be 6-8, a first organic layer is obtained after standing, and the first organic layer is distilled to obtain an intermediate 2; 3, the intermediate 2 and urea are subjected to an aldimine condensation reaction, and then a crude product of 5-fluorocytosine is obtained. According to the method, the synthesis process is simple, there are a few required reaction steps, the total yield is relatively high, the safety of reaction is high, the production efficiency is improved, and the production cost is reduced.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical chemical synthesis, and in particular relates to a preparation method of 5-fluorocytosine. Background technique

[0002] 5-Fluorocytosine, also known as flucytosine, 5-fluorocytidine, Ancozhi, and Anla spray, is a white or off-white crystalline powder, which is mainly used to treat fungal infections caused by cryptococcus and candida , such as fungal sepsis, endocarditis, meningitis, mucocutaneous candidiasis, candidal endocarditis, candidal arthritis, cryptococcal meningitis, and chromomycosis. This product is the drug of choice for the treatment of severe systemic albicans and cryptococcal infections in foreign countries, and it is used for the treatment of fungal meningitis, fungal respiratory tract infection and black mycosis.

[0003] In addition to being an antibacterial drug itself, 5-fluorocytosine is also the main intermediate for the preparation of capecitabine. Capecitabine can...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More