首页> 外国专利> PREPARATION METHOD FOR (R)-9-2-(PHOSPHONOMETHOXY)PROPYLADENINE WITH HIGH PURITY

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

机译:高纯度(R)-9-2-(光甲氧基)丙炔的制备方法

摘要

The present invention relates to a method for preparing (R)-9-[2-(phosphonomethoxy)propyl]adenine (PMPA) with high purity. The method includes easy processing steps and uses, as an intermediate, (diethoxyphosphoryl)methyl naphthalen-2-sulfonate or (diethoxyphosphoryl)methyl naphthalen-2-sulfonate generating little impurities to provide high purity. Thus, it is possible to obtain PMPA with high purity. Particularly, (diethoxyphosphoryl) methyl naphthalen-1-sulfonate is a solid material, is handled with ease during the use for preparation of PMPA, is suitable for mass production, allows production with uniform and constant quality, and thus can be introduced in a precise equivalent amount during the reaction. In addition, the method uses no reagent 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 significantly high purity. Thus, when such PMPA is used, it is possible to obtain tenofovir disoproxil and acid addition salts thereof with high purity, thereby facilitating production of high-quality material medicine.
机译:本发明涉及高纯度的(R)-9- [2-(膦酰基甲氧基)丙基]腺嘌呤(PMPA)的制备方法。该方法包括容易的加工步骤,并且使用(二乙氧基磷酰基)萘-2-磺酸甲酯或(二乙氧基磷酰基)萘-2-磺酸甲酯作为杂质,几乎不产生高纯度。因此,可以获得高纯度的PMPA。特别地,(二乙氧基磷酰基)萘-1-磺酸甲酯是固体材料,在用于制备PMPA的过程中易于处理,适合于批量生产,允许以均匀且恒定的质量进行生产,因此可以精确地引入。反应期间的当量。另外,该方法不使用对与水分和空气接触敏感的试剂,因此是安全的,显示出高再现性,并且适合于批量生产。此外,通过根据本发明的方法获得的PMPA具有明显高的纯度。因此,当使用这样的PMPA时,可以获得高纯度的替诺福韦二oproxil及其酸加成盐,从而有助于生产高质量的原料药。

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