Preparation methods of tenofovir disoproxil and fumarate thereof

2016 
The invention discloses preparation methods of tenofovir disoproxil and fumarate thereof, and belongs to the field of preparation of compounds. The methods comprise the following steps: carrying out a condensation reaction of a tenofovir anhydrous substance or tenofovir hydrate with chloromethyl isopropyl carbonate to obtain a reaction liquid, pouring the reaction liquid obtained from the condensation reaction into supersaturated salt water, stirring, filtering, washing, and drying to obtain a tenofovir disoproxil crude product; adding the tenofovir disoproxil crude product into a certain amount of a nonpolar organic solvent with low boiling point, heating up to a reflux temperature, carrying out beating reflux, then carrying out gradient cooling and stirring, filtering, washing the obtained product with a certain amount of the nonpolar organic solvent with low boiling point, and drying, to obtain powdered tenofovir disoproxil; and in the presence of isopropyl alcohol, carrying out a reaction of the powdered tenofovir disoproxil with fumaric acid to obtain the tenofovir disoproxil fumarate. The method has the advantages of simple post treatment and high yield, and the obtained product has the characteristics of high purity, low impurity content and the like.
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