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Method for preparing acyclovir

A production process, the technology of diacetyl acyclovir, applied in the field of pharmaceuticals, can solve the problems of low product quality, expensive raw materials, difficult product separation, etc., and achieve the effects of improving product quality, simple post-processing, and reducing costs

Inactive Publication Date: 2018-11-16
ZHEJIANG ZHEBEI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the continuous research of the predecessors, the production process of acyclovir is becoming more and more mature, but there are still the following problems: the raw materials are expensive, toxic reagents are used, the product quality is low, the yield is low, and the product separation is difficult
These problems have brought many difficulties to the industrialized production of acyclovir

Method used

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Examples

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Embodiment Construction

[0015] The technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Apparently, the described embodiments are only some of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0016] In Example 1 of the present invention, a manufacturing process of acyclovir specifically comprises the following steps:

[0017] S1. Synthesis of diacetylguanine: add guanosine, acetic anhydride, and boric acid into the reaction kettle at a weight ratio of 1:6.4:0.006, heat up to 110°C, and keep warm for 6 hours; then cool down to 60°C and keep warm for 6 hours to react End; then part of the reaction solution (40% of the feed amount) is distilled off under reduced pres...

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PUM

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Abstract

The invention discloses a method for preparing acyclovir, comprising synthesis of diacetylguanine, namely guanosine, acetic anhydride and boric acid are added to a reaction kettle at a weight ratio of1:6.4:0.006, the temperature is increased to 110-120 DEG C, and heat preservation is conducted for 6-12 hours; then the temperature is reduced to 60-100 DEG C, and heat preservation is conducted for6 hours, so the reaction is finished; subsequently, a part of the reaction liquid is distilled off under reduced pressure, the temperature is lowered to 3-5 DEG C to be maintained for 5 hours, discharging and centrifugal separation are conducted, rinsing with acetic anhydride is conducted for 3 times, and drying is conducted to obtain diacetylguanine. The method for preparing acyclovir provided bythe invention has the advantages that the process is easy to feed, the post-treatment is simple, the cost of the three-waste treatment is reduced, and ethanol is used as a recrystallization solvent,which not only reduces the cost, but also improves the product quality.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a preparation process of acyclovir. Background technique [0002] Acyclovir is a synthetic purine nucleoside analogue. It is mainly used for various infections caused by herpes simplex virus, and can be used for initial or recurrent skin, mucous membrane, external genital infection and HSV infection in immunocompromised persons. It is the drug of choice for the treatment of HSV encephalitis, and it is superior to adenosine vidarabine in reducing morbidity and mortality. It can also be used for herpes zoster, Epstein-Barr virus, and immunodeficiency complicated by chickenpox and other infections. For topical use on the skin only, acyclovir has less skin absorption. [0003] In the continuous research of the predecessors, the production process of acyclovir is becoming more and more mature, but there are still the following problems: the raw materials are expensive, toxic reagents are us...

Claims

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Application Information

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IPC IPC(8): C07D473/18
CPCC07D473/18
Inventor 谭梓骏王国华金琪谈国军倪建中黄伟强戴恩锋佘国荣全自力茹凯
Owner ZHEJIANG ZHEBEI PHARM CO LTD
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