Preparation method of acyclovir

Abstract

The invention discloses a preparation method of acyclovir, and belongs to the field of organic compound synthesis. According to the method, guanosine is taken as a starting raw material and is subjected to reactions of acylation, condensation and hydrolysis to prepare the acyclovir. Compared with the prior art, the synthesis method has stable and abundant raw material sources, market fluctuation influences are small, reaction conditions are mild, the operation is simple and safe, the reaction yield is high, the production cost is low, three wastes are few, and greater implementation value and socioeconomic benefits are provided.

Description

technical field [0001] The invention relates to a synthesis process of acyclovir, which belongs to the field of organic synthesis. Background technique [0002] Acyclovir (ACV), also known as acyclovir, English name acyclovir, chemical name 9-[(2-hydroxyethoxy)methyl]-guanine, is an efficient broad-spectrum antiviral drug , which was first synthesized and applied in the UK in 1981, has now been included in my country's national basic therapeutic drugs, and has a large market demand. The drug is highly effective against type I and type II herpes simplex and varicella zoster virus. With the deepening of people's research, this type of drug can also be applied to anti-HIV virus. [0003] The research on the synthetic method and production process of acyclovir has always been paid attention to by people, and there are multiple synthetic methods so far: [0004] 1) Using 2-chloro-6-iodopurine as raw material, first condense with trimethylsiloxyethyl iodomethyl ether to generate ...

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Problems solved by technology

[0005]2) Using 2,6,9 silanized guanine as raw material, and 2-oxa-1,4-butanediol diethyl ester (OBDDA ), under the catalysis of iodine and phosphate, it condenses into a 9-position substituted product, and then hydrolyzes the product with a yield of 35%, which is relatively low

[0006]3) Using guanine as a raw material, first undergo acetylation to generate N2, N9-diacetyl Guanine (DAG), and then condensed with 2-oxa-1,4-butanediol diethyl ester to generate diacetyl acyclovir (DACV), and then hydrolyzed to obtain the target product, but the 7-position will be generated during the condensation process Diacetyl acyclovir (7-DACV), increases the difficulty of product purification, affects the stability of product yield and product quality

[0008] Although the production process of acyclovir is becoming more and more mature, it is a pity that the following problems generally exist in the existing process: expensive raw materials, use of toxic reagents, reaction Strict conditions, low product quality, low yield, difficult product separation and purification, etc.

The above drawbacks make the synthetic technique of acyclovir bulk drug difficult to suitability for suitability for industrialized production

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