1244022-53-4

Usage

Uses

Used in Pharmaceutical Industry:
6N-HydroxyMethyl Tenofovir Disoproxil is used as an intermediate for the synthesis of Tenofovir Disoproxil Fumarate (T018505) for its antiviral properties. It is particularly effective against HIV and Hepatitis B, making it a valuable component in the development of medications for these viral infections.
Used in Antiviral Medication:
6N-HydroxyMethyl Tenofovir Disoproxil is used as a key component in the production of antiviral drugs, specifically Tenofovir Disoproxil Fumarate (T018505). This medication is prescribed for the treatment of HIV and Hepatitis B, helping to control the viral load and prevent the progression of these diseases.
Used in Research and Development:
6N-HydroxyMethyl Tenofovir Disoproxil is also utilized in the research and development of new antiviral therapies. Its chemical properties and role in the synthesis of Tenofovir Disoproxil Fumarate make it an essential compound for scientists and researchers working on innovative treatments for viral infections.

Upstream product

• 50-00-0 formaldehyd 
• 201341-05-1 tenofovir disoproxil 
• 180587-75-1 (R)-diethyl (((1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonate 
• 14047-28-0 (R)-9-(2-hydroxypropyl)adenine 
• 66224-66-6 adenine 
• 35180-01-9 chloromethyl isopropyl carbonate 
• 147127-20-6 tenofovir 

Relevant academic research and scientific papers

Preparation process of tenofovir disoproxil fumarate impurities

A preparation process of tenofovir disoproxil fumarate impurities is provided. The invention discloses a synthesizing method of 2 tenofovir disoproxil fumarate impurities, wherein the two impurities have the structures of a compound represented by the formula I and a compound represented by the formula II; with tenofovir disoproxil fumarate as a raw material, the impurities are obtained by carrying out a reaction of the tenofovir disoproxil fumarate with paraformaldehyde in a reaction solvent; the compound represented by the formula I and the compound represented by the formula II are both used as reference substances for detection of tenofovir disoproxil fumarate related substances, and are helpful to control of the quality of the tenofovir disoproxil fumarate and control of the preparation purity.

Process improvements for the manufacture of tenofovir disoproxil fumarate at commercial scale

The three-step manufacturing process used in the synthesis of tenofovir disoproxil fumarate (1) was studied and optimized, leading to a more productive and robust process. The yield was improved from about 13% overall to 24%. Key process improvements identified included implementation of a telescoped process for the second stage that obviated the need for an extraction and solvent exchange, and significant optimization of the final reaction, including the beneficial effect of adding a quaternary ammonium salt to the alkylation reaction and development of a nonaqueous process for removal of NMP and triethylamine from the product mixture to decrease the level of decomposition of product during the isolation.