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    • 6. 发明授权
    • Preparation of optically active azole derivatives
    • 光学活性唑衍生物的制备
    • US4774338A
    • 1988-09-27
    • US856913
    • 1986-04-28
    • Uwe Priesnitz
    • Uwe Priesnitz
    • A01N43/50A01N43/653C07B31/00C07B57/00C07C67/00C07D233/60C07D233/61C07D249/08C07D521/00
    • C07D231/12C07D233/56C07D249/08
    • A process for the preparation of a substantially pure optically active azole derivative of the formula ##STR1## in which R.sup.1 and R.sup.3 are organic radicals,R.sup.2 is hydrogen or methyl, andX is N or CH,comprising in a first stage reacting a racemate of an azole derivative of the formula ##STR2## with an optically active permethric acid halide of the formula ##STR3## in which Hal represents chlorine or bromine,thereby to produce a diastereomeric mixture of an ester of the formula ##STR4## in a second stage separating the components of the ester mixture based on their different physical properties, and in a third stage reacting an individual component ester with a base in the presence of a diluent to liberate the desired substantially pure optically active azole derivative.
    • 制备式“IMAGE”的基本上纯的光学活性唑衍生物的方法,其中R 1和R 3是有机基团,R 2是氢或甲基,X是N或CH,包括在第一阶段中使外消旋物 具有式“IMAGE”的光学活性二氯甲基卤,其中Hal表示氯或溴,由此在第二级分离中产生式“IMAGE”的酯的非对映体混合物 基于它们不同物理性质的酯混合物的组分,以及在稀释剂存在下使单独组分酯与碱反应的第三阶段,以释放所需的基本上纯的光学活性唑衍生物。