Acyclovir Raw Materials Powder CAS 59277-89-3

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Acyclovir Raw Materials 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 for the skin, skin absorption is less.

1,herpes simplex virus infection: oral for genital herpes virus infection in primary and recurrent cases, for recurrent cases of oral use of the product as a prophylactic. Injections are used for immunodeficient persons. It is used for the treatment of primary and recurrent mucocutaneous infections as well as prophylaxis of recurrent cases; it is also used for the treatment of herpes simplex encephalitis.

2,herpes zoster: oral for immunocompetent people with herpes zoster and immunodeficient people mild cases of treatment. Injections are used for the treatment of severe cases of herpes zoster in immunodeficient persons.

3,Treatment of chickenpox in immunodeficient persons.

4,Topical use for early genital herpes infections caused by herpes simplex virus and self-limited mucocutaneous herpes simplex in immunodeficient persons in primary and recurrent cases.

5,With its sodium salt for the treatment of acute retinal necrosis. Nucleotide antivirals for the treatment of:

(1) Herpes simplex keratitis;

(2) Herpes simplex;

(3) Herpes zoster;

(4) Treatment of acute retinal necrosis with its sodium salt. It is mainly used for superficial and deep keratitis caused by herpes simplex virus and herpes zoster virus.

Uses and functions of Acyclovir Powder.

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 used clinically for herpes simplex virus encephalitis, herpes virus keratitis and external genital infections, varicella zoster virus infection and cytomegalovirus infection in AIDS, and chronic hepatitis B. It is also used as an antimetabolite.

A guanosine analogue that acts as an antimetabolite.

Pharmacological Effects of Acyclovir Raw Powder.

Antiviral. In vitro inhibitory effect on herpes simplex virus, varicella zoster virus and cytomegalovirus. The product enters the herpes virus-infected cells and competes with deoxyriboside for viral thymidine kinase or cellular kinase, and the drug is phosphorylated into activated acyclovir triphosphate, which then inhibits viral replication in two ways:

1, interfering with viral DNA polymerase and inhibiting viral replication;

2, binding to the growing DNA strand under the action of DNA polymerase, causing interruption of DNA strand elongation.　The product has a special affinity for viruses, but has low toxicity to mammalian host cells. Carcinogenicity has been reported in in vitro cell transformation assays, but no basis for carcinogenicity has been seen in animal studies. Some animal studies have shown mutagenicity at high concentrations, but there is no basis for chromosomal changes.

Production method of Acyclovir.

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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