What is Tenofovir? What is its purpose?

Category: Industry Update

Time: 2025-05-19

Summary: Tenofovir, also known as tenofovir, is (R) -9- (2-methoxypropyl phosphate) - adenine, an antiviral drug for AIDS.

Tenofovir, also known as tenofovir, is (R) -9- (2-methoxypropyl phosphate) - adenine, an antiviral drug for AIDS. Tenofovir is also a key intermediate of tenofovir fumarate (II), an antiviral drug for AIDS with better effect. Because tenofovir, especially tenofovir fumarate, has good anti AIDS activity, it is widely used in clinic.
Function
The approved indication is the combination therapy with other antiretroviral drugs for the treatment of HIV-1 infection. Tenofovir is the first nucleotide analogue approved for the treatment of HIV-1 infection. The mechanism by which nucleotide analogues block HIV replication is similar to that of nucleotide analogues.
Preparation method
Under nitrogen protection, dissolve diethyl phosphite, polyformaldehyde, and triethylamine in toluene, react at 87 ℃, and then reflux. After the reaction is complete, cool to 1 ℃ and slowly add p-toluenesulfonyl chloride and triethylamine to a temperature not exceeding 10 ℃. After addition, react at 22 ℃ to obtain diethyl p-toluenesulfonyloxymethylphosphonate.
Under nitrogen protection, (S) - glycidol, 5% palladium charcoal, ethanol, and sodium hydroxide aqueous solution were mixed and hydrogenated to obtain (R) -1,2-propanediol. Add ethanol solution of diethyl carbonate and sodium ethoxide, and react to obtain (R) -1,2-propanediol carbonate. Dissolve it with adenine, diethyl p-toluenesulfonyloxymethylphosphonate, and sodium hydroxide in dimethylformamide, and react until complete at 130 ℃ to obtain (R) -9 [2- (diethylphosphonomethoxy) propyl] adenine.
Dissolve it in acetonitrile, add bromotrimethylsilane, reflux until complete, and obtain crude Tenofovir, which can be recrystallized from water. After stirring Tenofovir with 1-methyl-2-pyrrolidone and triethylamine, chloromethyl 2-propyl carbonate was added and reacted at 55-65 ℃ until complete. Then, it was acidified with fumaric acid to obtain Tenofovir fumarate dipentenoyloxymethyl ester.

Keywords: What is Tenofovir? What is its purpose?

Blogs

Knowledge