C(SP3)-C(SP2) CROSS-COUPLING REACTION OF ORGANOZINC REAGENTS AND HETEROCYCLIC (PSEUDO)HALIDES
    4.
    发明申请
    C(SP3)-C(SP2) CROSS-COUPLING REACTION OF ORGANOZINC REAGENTS AND HETEROCYCLIC (PSEUDO)HALIDES 审中-公开
    C(SP3)-C(SP2)有机锌试剂与杂环(假)卤代物的交叉偶联反应

    公开(公告)号:WO2018019291A1

    公开(公告)日:2018-02-01

    申请号:PCT/CN2017/094898

    申请日:2017-07-28

    发明人: YAN, He ZHAO, Jingbo

    摘要: Provided is a method of synthesizing a C(sp 3 )-C(sp 2 ) cross-coupled compound comprising reacting a C(sp 3 ) coupling partner with a C(sp 2 ) coupling partner, a catalyst, and a solvent; wherein the C(sp 3 ) coupling partner comprises an organic zinc reagent; and wherein the C(sp 2 ) coupling partner comprises a heterocyclic halide or a heterocyclic pseudo halide. The method further comprises synthesis of the organic zinc reagent, wherein the synthesis comprises reacting a zinc powder with an acid, filtering, washing, and drying to obtain an activated zinc powder; and reacting the activated zinc powder with a metal iodide catalyst and a second solvent and heating for a predetermined time to obtain the organic zinc reagent.

    摘要翻译: 提供了合成C(sp 3)-C(sp 2 2)交叉偶联化合物的方法,其包括使C(sp 3)偶联配偶体与C(sp 2)偶联配偶体,催化剂和溶剂接触; 其中C(sp 3 3)偶联配偶体包含有机锌试剂; 并且其中C(sp 2 2)偶联配偶体包含杂环卤化物或杂环假卤化物。 该方法还包括有机锌试剂的合成,其中合成包括使锌粉与酸反应,过滤,洗涤并干燥,得到活性锌粉; 使活性锌粉与金属碘化物催化剂和第二溶剂反应并加热预定时间以获得有机锌试剂。