Process for the preparation of Tenofovir

摘要

The present invention provides a process for the preparation of tenofovir. The present invention also provides a process for the preparation of tenofovir disoproxil or a salt thereof and its pharmaceutical composition using the tenofovir of the present invention.

主权项

1. A process for the preparation of tenofovir of formula I, comprising the steps of: a) reacting 9-[2-(R)-(hydroxy)propyl]adenine (HPA) of formula III with di-Alk-p-toluene sulfonyloxy methyl phosphonate in presence of a base and a metal salt in an organic solvent to obtain (R)-9-[2-(di-Alk-phosphono methoxy)propyl]adenine of formula II; wherein “Alk” represents C1-4 alkyl, and wherein the metal salt is represented by the formula MX2, wherein M represents a divalent metal cation, and X represents halide, acetate, or trifluoromethane sulfonate; and b) dealkylating the compound of formula II with a suitable dealkylating agent to obtain tenofovir.