Process for Preparation of Cyclic Prodrugs of PMEA and PMPA
    3.
    发明申请
    Process for Preparation of Cyclic Prodrugs of PMEA and PMPA 审中-公开
    制备PMEA和PMPA循环前药的方法

    公开(公告)号:US20070203339A1

    公开(公告)日:2007-08-30

    申请号:US11670806

    申请日:2007-02-02

    IPC分类号: C07F9/655 C07D263/04

    CPC分类号: C07F9/657181

    摘要: The method of preparing compounds of Formula I is described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1-2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising: coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with MPOCl2 or an N-6 substituted analogue thereof. Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

    摘要翻译: 描述了制备式I化合物的方法:其中:M和V彼此是顺式的,MPO 3 H 2是选自以下的膦酸: 9-(2-膦酰基甲氧基乙基)腺嘌呤和(R)-9-(2-膦酰基甲氧基丙基)腺嘌呤; 其中V是苯基,任选被1-2个选自氟,氯和溴的取代基取代; 包括:将其中苯基可以任选取代的手性1-苯基丙烷-1,3-二醇与MPOCl 2 N或其N-6取代的类似物偶联。 另外,描述了能够分离和纯化所需异构体的方法和盐形式。