1246812-40-7Relevant articles and documents
Synthesis method of tenofovir disoproxil fumarate impurity
-
Paragraph 0021; 0023-0025; 0027; 0028-0029; 0031-0032, (2019/11/12)
The invention relates to a synthesis method of a tenofovir disoproxil fumarate impurity. The tenofovir disoproxil fumarate impurity is (R)-[[2-(6-amino-9H-purine-9-radical)-1-methylethoxy]methyl]-(isopropoxy)-phosphoric acid isopropoxy carbonyl oxymethyl ester, and is prepared by using T-A:(R)-(1-(6-amino-9H-purine-9-radical)propyl-2-radical)oxygroup) methyl)phosphonic acid, N,N-diisopropylethylamine (DIPEA) and 1-(3-dimethyl amino propyl)-3-ethyl carbon diimine hydrochloride (EDC.HCL) as starting materials and two processes of esterification reaction and condensation reaction. According to the synthesis method, reaction raw materials are relatively readily available, the reaction process is easy to operate, requirements on reaction equipment are low, the reaction condition is relatively mild, the yield and purity are high, the cost is saved, and the synthesis method has great acceleration effect on more in-depth and extensive research of related drug use safety, reliability and stability of tenofovir disoproxil fumarate and quality control in the production process.