PREPARATION METHOD FOR (R)-9-2-(PHOSPHONOMETHOXY)PROPYLADENINE WITH HIGH PURITY

摘要

The present invention relates to a method for preparing (R)-9-[2-(phosphonomethoxy)propyl]adenine (PMPA) with high purity. The method uses crystalline (dimethoxyphosphoryl)methyl naphthalene-1-sulfonate requiring an easy reaction process, producing a low amount of impurities during reaction and having high purity, as an intermediate. Thus, it is possible to obtain PMPA having high purity. Particularly, (dimethoxyphosphoryl)methyl naphthalene-1-sulfonate is a solid material and is handled with ease, when used for preparing PMPA, is suitable for mass production and is obtained with uniform and constant quality, and thus can be introduced in an accurate equivalent amount during reaction. In addition, the method uses no reagents sensitive to contact with moisture and air, and thus is safe, shows high reproducibility and is suitable for mass production. Further, PMPA obtained by the method according to the present invention has very high purity, and thus use of such PMPA allows production of tenofovir disoproxil and an acid addition salt thereof with high purity. Therefore, the PMPA is useful for producing high-quality active pharmaceutical ingredients.