Synthesis method of 6-ethyl-4-hydroxyl-5-fluorine-2-cloro pyridine ammonium salt

A technology of chloropyrimidine ammonium salt and synthesis method, which is applied in the field of synthesis of 6-ethyl-4-hydroxy-5-fluoro-2-chloropyrimidine ammonium salt, and can solve the problem of poor oxidation effect compared to iodine, low yield waste liquid, etc. problems, to avoid the use of format reagents and iodine, good product quality, and low production costs
CN101671309BActive Publication Date: 2011-07-20上海永阔生物医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
上海永阔生物医药科技有限公司
Publication Date
2011-07-20

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Abstract

The invention discloses a synthesis method of 6-ethyl-4-hydroxyl-5-fluorine-2-cloro pyridine ammonium salt with a structure showed as a formula (I), comprising the following steps: taking 2-fluorine-3-oxo valerate as a starting material, and condensing with O-methylisourea in alcoholic solution of sodium alcoholate to prepare an intermediate (II); carrying out acid-catalyzed hydrolysis on the intermediate (II) to prepare an intermediate (III); carrying out chlorinated reaction on the intermediate (III) by adopting chlorinated reagent to prepare a compound (IV); and preparing an intermediate (V) by the compound (IV) in alkaline water solution through hydroxyl substitution, and ammoniating the intermediat (V) by ammonia water to form salt, namely, obtaining the 6-ethyl-4-hydroxyl-5-fluorine-2-cloro pyridine ammonium salt. The synthesis method adopts cheap and easily-obtained starting raw material, avoids the use of format reagent and iodine, simplifies operations, reduces environmentalpollution, is beneficial to industrial production and has lower production cost and good product quality.
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Description

Technical field

[0001] The invention specifically relates to a method for synthesizing the intermediate 6-ethyl-4-hydroxy-5-fluoro-2-chloropyrimidine ammonium salt (hereinafter referred to as EFCP) of the antifungal drug voriconazole. Background technique

[0002] Antifungal drugs are a class of essential drugs that have been vigorously developed in countries around the world in recent years. In recent years, due to the widespread application of cytotoxic drugs, immunosuppressants, broad-spectrum antibiotics, the development of treatment methods such as organ transplantation, catheter technology, intravenous hypernutrition, and clinical serious diseases such as tumors, blood diseases, AIDS, diabetes, and senile diseases The morbidity of AIDS continues to rise, making deep fungal infections on the rise, especially cancer and AIDS patients are extremely susceptible to fungal infections. In recent years, triazole antifungal drugs have stronger antibacterial activity and lower toxic...

Claims

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