Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Preparation method of flucytosine

A technology of flucytosine and cytosine, which is applied in the field of pharmaceutical chemical synthesis, can solve the problems of cumbersome preparation process and poor medicinal effect of flucytosine, and achieve the effects of simple production steps, remarkable therapeutic effect and low raw material cost

Inactive Publication Date: 2021-10-29
德州隆盛化工有限公司
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current flucytosine has poor medicinal properties, and the preparation process is relatively cumbersome

Method used

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
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A method for preparing flucytosine, comprising the following steps:

[0027] S1: Material preparation:

[0028] Prepare organic base: 2 parts, organic base is one of xylene and carbon tetrachloride, cytosine: 1 part, halogenation reagent: 2 parts, halogenation reagent is liquid bromine, copper bromide One of them, amino-protecting agent: 0.5 parts, amino-protecting agent is one of di-tert-butyl dicarbonate, benzyl chloroformate, chloroformic acid-P-fluorenic acid, fluorinated reagent: 1 part, aztreonam: 2 servings, compound probiotics: 0.5 servings, compound probiotics contain Bifidobacterium longum, Lactobacillus bulgaricus and Streptococcus thermophilus;

[0029] S2: Preparation One:

[0030] Take 2 parts of organic base and put it into a reaction kettle with a temperature of 80°C, then take 1 part of cytosine and 2 parts of halogenation reagent, put the taken cytosine and halogenation reagent into the reaction kettle and mix with organic base Stirring, the stirrin...

Embodiment 2

[0037] A method for preparing flucytosine, comprising the following steps:

[0038] S1: Material preparation:

[0039] Prepare organic base: 12 parts, organic base is one of xylene and carbon tetrachloride, cytosine: 10 parts, halogenation reagent: 8 parts, halogenation reagent is liquid bromine, copper bromide One of them, amino-protecting agent: 5 parts, amino-protecting agent is one of di-tert-butyl dicarbonate, benzyl chloroformate, chloroformic acid-P-fluorenic acid, fluorine reagent: 5 parts, aztreonam: 9 servings, compound probiotics: 6 servings, compound probiotics contain Bifidobacterium longum, Lactobacillus bulgaricus and Streptococcus thermophilus;

[0040] S2: Preparation One:

[0041] Take 12 parts of organic base and put it into a reaction kettle with a temperature of 80°C, then take 10 parts of cytosine and 8 parts of halogenation reagent, put the taken cytosine and halogenation reagent into the reaction kettle and mix with organic base Stirring, the stirrin...

Embodiment 3

[0048] A method for preparing flucytosine, comprising the following steps:

[0049] S1: Material preparation:

[0050] Prepare organic base: 3 parts, organic base is one of xylene and carbon tetrachloride, cytosine: 2 parts, halogenation reagent: 3 parts, halogenation reagent is liquid bromine, copper bromide One of them, amino-protecting agent: 0.6 parts, amino-protecting agent is one of di-tert-butyl dicarbonate, benzyl chloroformate, chloroformic acid-P-fluorenic acid, fluorine reagent: 2 parts, aztreonam: 3 servings, compound probiotics: 0.6 servings, compound probiotics contain Bifidobacterium longum, Lactobacillus bulgaricus and Streptococcus thermophilus;

[0051] S2: Preparation One:

[0052] Take 3 parts of organic base and put it into a reaction kettle with a temperature of 80°C, then take 2 parts of cytosine and 3 parts of halogenation reagent, put the taken cytosine and halogenation reagent into the reaction kettle and mix with organic base Stirring, the stirrin...

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

PUM

No PUM Login to View More

Abstract

The invention discloses a preparation method of flucytosine. The preparation method comprises the following steps of S1, material preparation: separately preparing 2-12 parts of organic alkali, 1-10 parts of cytosine, 2-8 parts of a halogenating reagent, 0.5-5 parts of an amino protective agent, 1-5 parts of a fluorinating reagent, 2-9 parts of aztreonam and 0.5-6 parts of compound probiotics; and S2, preparation I: putting a certain amount of organic alkali into a reaction kettle at the temperature of 80 DEG C, then taking a certain amount of cytosine and a certain amount of halogenating reagent, putting the taken cytosine and halogenating reagent into the reaction kettle, and mixing and stirring with the organic alkali to obtain an intermediate I. According to the flucytosine preparation method, the preparation steps are simple, unnecessary tedious steps are omitted, the raw material cost is low, the product quality is very stable, the treatment effect can be improved and is more remarkable through the added aztreonam, the nutritional ingredients can be increased through the added compound probiotics, and the side effects can be reduced.

Description

technical field [0001] The invention relates to the technical field of medicinal chemical synthesis, in particular to a preparation method of flucytosine. Background technique [0002] Flucytosine is used for the treatment of fungal infections caused by cryptococcus and candida, such as fungal sepsis, endocarditis, meningitis, and lung and urinary tract infections. Antifungal drugs are mainly used for skin and mucous membrane candidiasis, Candida endocarditis, candida arthritis, cryptococcal meningitis, and chromomycosis; however, blood phase should be checked regularly during the medication period, and patients with hepatic and renal insufficiency and blood diseases and pregnant women should use it with caution, and patients with severe renal insufficiency are contraindicated. The current flucytosine has poor medicinal properties, and the preparation process is relatively cumbersome. Therefore, we propose a preparation method of flucytosine. Contents of the invention ...

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

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505C07D239/47A61P31/10A61K35/744A61K35/745A61K35/747
CPCC07D239/47A61K31/505A61P31/10A61K35/745A61K35/747A61K35/744
Inventor 明德志
Owner 德州隆盛化工有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com