1246812-40-7Relevant academic research and scientific papers
Tenofovir disoproxil fumarate analog preparation method
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Paragraph 0010; 0030; 0031, (2019/03/10)
The present invention discloses a tenofovir disoproxil fumarate analog preparation method, which comprises: carrying out a substitution reaction on adenine as a raw material and (R)-propylene carbonate in the presence of an alkali, carrying out a substitution reaction with (diethoxyphosphoryl)methyl-4-methylbenzenesulfonate, hydrolyzing with a concentrated hydrochloric acid solution, crystallizingto obtain anhydrous tenofovir, carrying out a reaction on the anhydrous tenofovir and chloromethyl isopropyl carbonate to obtain tenofovir monoester, and carrying out a reaction with 2-bromopropane to obtain the target compound. According to the present invention, the selected starting raw materials are inexpensive and easy to obtain, the process is simple, and the material utilization rate and total yield are improved; and the intermediate of the method is purified by re-crystallization, such that the yield is high, and the purity is high.
Synthesis method of tenofovir disoproxil fumarate impurity
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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.
