Method for enantioselective preparation of sulphoxide derivatives
    4.
    发明授权
    Method for enantioselective preparation of sulphoxide derivatives 失效
    亚砜衍生物的对映选择性制备方法

    公开(公告)号:US07528251B2

    公开(公告)日:2009-05-05

    申请号:US11663647

    申请日:2005-10-05

    IPC分类号: C07D471/04

    摘要: The present invention concerns enantioselective preparation of sulphoxide derivatives or their salts. The method consist in performing an enantioselective oxidation of a sulphur of general formula (I) A —CH2—SB, wherein: A is a diversely substituted pyridinyl ring and B is a heterocyclic radical comprising an imidazo-pyridinyl ring, using an oxidizing agent in the presence of a titanium (IV)-based catalyst and a chiral ligand consisting of a cyclic beta or gamma-amino-alcohol, in an organic solvent, followed, if required, by salt formation with a base. The invention is useful for preparing sulphoxides useful in therapeutics.

    摘要翻译: 本发明涉及亚砜衍生物或其盐的对映选择性制备。 该方法包括对通式(I)A -CH 2 -SB的硫进行对映选择性氧化,其中:A是不同取代的吡啶环,B是包含咪唑并吡啶环的杂环基,使用氧化剂 在有机溶剂中存在基于钛(IV)的催化剂和由环状β或γ-氨基醇组成的手性配体,如果需要,则与碱形成盐。 本发明可用于制备用于治疗的亚砜。