Synthesis method and application of voriconazole

Abstract

The invention belongs to the field of drug synthesis and discloses a synthesis method and application of voriconazole. The synthetic method of voriconazole provided by the present invention is (2R,3S)-2-(2,4-difluorophenyl)-3-(4-chloro-5-fluoropyrimidin-4-yl)-1-(1H ‑1,2,4‑triazole‑1‑yl)‑2‑butanol is dechlorinated and reduced under acidic conditions to generate voriconazole. The voriconazole tablets were prepared through steps such as tablet compression and coating. The invention can improve the yield of voriconazole and reduce the production cost on the basis of ensuring the purity of voriconazole; the prepared voriconazole tablets also have high dissolution rate of voriconazole and have good medical effect. The invention is suitable for the synthesis of voriconazole and the preparation of voriconazole tablets, especially for the synthesis of voriconazole with high yield and the preparation of voriconazole tablets with high dissolution rate.

Description

Synthetic method and application of voriconazole technical field The invention belongs to the field of drug synthesis, relate to the synthetic method and application of voriconazole, specifically a kind of high yield Synthetic method and application of efficient voriconazole. Background technique Voriconazole (Voriconazole) is a kind of new synthetic on the structural basis of fluconazole by American Pfizer. The broad-spectrum triazole antifungal drug has the advantages of good pharmacokinetic characteristics and broad antibacterial spectrum, and has become an invasive First-line treatment for aspergillosis with the chemical name (2R,3S)‑2‑(2,4‑difluorophenyl)‑3‑(5‑fluoropyrimidine‑4‑yl)‑ 1-(1H-1,2,4-triazole-1-base)-2-butanol, its structural formula is as follows: [0003] At present, the system of synthesizing voriconazole in the prior art is all under strong alkaline conditions, and it is easy to cause voriconazole The hydrolysis of conazole makes the purifica...

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Problems solved by technology

[0004] At present, the systems for synthesizing voriconazole in the prior art are all under strong alkaline conditions, which easily cause the hydrolysis of voriconazole, making the purification of voriconazole difficult and the yield reduced. In order to achieve the standard purity of the preparation of drugs, it is often necessary to prepare a large amount of voriconazole , This undoubtedly increases the production cost of the enterprise and causes a large amount of waste in the preparation of raw materials, so it is very necessary to develop a high-yield voriconazole synthetic method

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