HRK Supply Tenofovir raw Materials powder

CAS:147127-20-6

MF:C9H14N5O4P

MW:287.21

EINECS:604-571-2

Specification​: 99% min Tenofovir Powder

Sample:Tenofovir Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:white

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Tenofovir Powder Usage and Synthesis.

Tenofovir is almost not absorbed through the gastrointestinal tract, so it is esterified and salted as Tenofovir ester fumarate. Tenofovir ester is water-soluble and can be rapidly absorbed and degraded into the active substance Tenofovir, which is then converted into the active metabolite Tenofovir bisphosphonate. Tenofoveda blood drug peak within 1 to 2 hours after administration. Tenofovir bioavailability increases by about 40% when taken with food. Tenofovir bisphosphonates have an intracellular half-life of about 10h and can be administered once a day. Because the drug is not metabolized by the CYP450 enzyme system, interactions with other drugs caused by this enzyme are highly unlikely. The drug is excreted mainly through the glomerular filtration and active tubule transport system, and about 70% to 80% is excreted in its original form through urine.

Uses of Tenofovir.

Nucleotide analogues reverse transcriptase inhibitors block HIV replication. It is used in combination with other antiretroviral drugs to treat HIV-1 infection. Used in the treatment of AIDS.

Preparation of Tenofovir.

Diethyl phosphite, paraformaldehyde and triethylamine were dissolved in toluene and reacted under nitrogen to reflux. After the reaction was complete, it was cooled and slowly added p-toluenesulfonyl chloride and triethylamine to obtain p-toluenesulfonyloxymethylphosphonate diethyl. Under the protection of nitrogen, (S) -glycidyl, 5% palladium  carbon, ethanol and sodium hydroxide aqueous solution were mixed and hydrogenated to obtain (R)-1, 2-propylene glycol. (R)-1, 2-propylene glycol carbonate was obtained by adding diethyl carbonate and sodium ethanol-ethanol solution.

It was dissolved in dimethylformamide with adenine, diethyl p-toluenesulfonyl methyl phosphonate and sodium hydroxide to obtain (R)-9- [2- (diethylphosphonyl methoxy) propyl] adenine. Dissolve it in acetonitrile, add bromo-trimethylsilane, detenofovir crude, recrystallized to obtain pure product. Tenofovir was mixed with 1-methyl-2-pyrrolidone and triethylamine to react with chloromethyl propyl carbonate, and then acidified with fumarate to obtain Tenofovir fumarate divaleryl methyl ester.

Product method of Bulk Tenofovir Powder.