ENANTIOMERIC RESOLUTION OF 2,4-DISUBSTITUTED 1,3-OXATHIOLANE NUCLEOSIDES
    1.
    发明申请
    ENANTIOMERIC RESOLUTION OF 2,4-DISUBSTITUTED 1,3-OXATHIOLANE NUCLEOSIDES 审中-公开
    2,4-取代的1,3-二氧杂环己烷核苷酸的完全分辨率

    公开(公告)号:US20120184739A1

    公开(公告)日:2012-07-19

    申请号:US13062236

    申请日:2008-09-05

    IPC分类号: C07D411/04

    CPC分类号: C07D327/04

    摘要: Single enantionmers of compounds of formula (B), in either the cis or trans configuration, wherein R1 and R2 are as defined herein, can be separated from enantiomeric mixtures thereof by reacting the compound with an acid to produce a conglomerate salt that has the following characteristics: the IR spectrum of the salt of the racemic compound, a 1:1 mixture of (−) and (+) crystals, is identical to that of the each of the single enantiomer, and the salt of the racemic compound has a melting point lower that that of either single enantiomer. The conglomerate salt is then separated by preferential crystallization.

    摘要翻译: 式(B)化合物的单一对映体,其顺式或反式构型,其中R 1和R 2如本文所定义,可以通过使该化合物与酸反应,从而与其对映异构体混合物分离,从而产生具有下列化合物的砾岩盐 特征:外消旋化合物的盐,( - )和(+)晶体的1:1混合物的IR光谱与单一对映异构体的相同,外消旋化合物的盐具有熔融 低于单一对映异构体。 然后通过优先结晶分离砾岩盐。