Tenofovir disoproxil fumarate
China [CN] Fumaric acid tenofovir is the Gilead listed companies to develop a kind of nucleotide antiviral drugs, in 2001, approved by the FDA for the treatment of human immunodeficiency virus (humanimmunodeficiencyvirus, HIV) infection. It was launched in the European Union in 2002 and approved for the treatment of HIV-1 and chronic hepatitis B. Tenofovir fumarate dipivoxil, as a nucleotide reverse transcriptase inhibitor, is an orally available open-loop nucleotide phosphate prodrug. After oral absorption, it rapidly converts into tenofovir to exert its therapeutic effect. Due to its high bioavailability, definite therapeutic effect and good tolerance, TDF has now become the recommended first-line anti-HIV drug with the highest sales. Patent literature reports the synthesis method of tenofovir fumarate ester, but there are problems such as excessive impurities in some intermediates, low optical purity, difficult operation, low yield, unqualified fumaric acid content and unsuitability for industrial production.
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