Antipyretic and analgesic raw materials Acyclovir Powder

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Acyclovir Powder Usage and Synthesis.

Acyclovir is a synthetic purine nucleoside antiviral, one of the most commonly used antiviral drugs, mainly used for a variety of infections caused by herpes simplex virus, can be used for primary or recurrent skin, mucous membrane, external genital infections and HSV infections occurring in immunodeficient individuals. It is the drug of choice for the treatment of HSV encephalitis, and is superior to adenosine in reducing morbidity and mortality. It is also used for herpes zoster, EBV, and chickenpox infections in immunodeficient individuals. Topical use only on the skin, with low skin absorption.

Acyclovir is a purine nucleoside derivative with inhibitory effect on DNA synthesis, and its anti-herpes virus activity is 160 times stronger than that of adenosine.

It is clinically used for herpes simplex virus encephalitis, herpes virus keratitis and external genital infections, varicella zoster virus infections and cytomegalovirus infections of AIDS, chronic hepatitis B, and so on.

Uses and functions of Acyclovir.

Acyclovir is a purine nucleoside derivative with inhibitory effect on DNA synthesis, and its anti-herpes virus activity is 160 times stronger than that of adenosine.

It is clinically used for herpes simplex virus encephalitis, herpes virus keratitis and external genital infections, varicella zoster virus infections and cytomegalovirus infections of AIDS, chronic hepatitis B, and so on.

Side Effects of Acyclovir.

It is generally well tolerated. Topical use has its mild irritant symptoms, and IV extravasation can cause local inflammation and phlebitis, as well as anorexia, nausea, headache and dermatitis.

Product Method of  Bulk Acyclovir Powder.

Method 1: Guanine was used as raw material. Guanine and acetic anhydride were mixed, a small amount of acetic acid and zinc acetate were added, and refluxed with stirring. Evaporate the excess of acetic anhydride under reduced pressure, cool to 0 ℃ and filter, the filter cake was washed with ethanol and water, dry, get N, N, -diacetyl guanine, yield 92.6%.

The acetic anhydride, acetic acid and p-toluenesulfonic acid were mixed and cooled to below 10 °C. Dioxopentane was added with stirring and the internal temperature was controlled below 40°C. Cool to room temperature, add toluene and N,N'-diacetyl guanosine and reflux with stirring.

Cool to room temperature, add chloroform and filter. The filter cake was washed with chloroform, dried and dissolved in 40% aqueous methylamine solution, stirring reflux. Cooling, filtration, filtrate concentrated to a slurry under reduced pressure, cooled and washed with ethanol, filtration.

The filter cake was recrystallised with water to obtain acyclovir, yield 75%, melting point 255-258 ° C. N, N'-diacetyl guanine can also be and 2-oxa-1,4-butanediol diacetate in dimethylsulfoxide, catalyzed by p-toluenesulfonic acid, the reaction was at 100 ° C, then chromatography to obtain the diacetate ester of acyclovir, and then in saturated ammonia in methanol solution Hydrolysis was carried out to obtain acyclovir with an overall yield of 43% in terms of guanine.

Method 2: After trimethylsilylation of guanine, and then reacted with 2-benzyloxyethoxymethyl chloride, and then removed the benzyl to get acyclovir, the yield was 24%.

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