Process for preparing A 2-substituted benzofuran-3-yl borate ester
    11.
    发明授权
    Process for preparing A 2-substituted benzofuran-3-yl borate ester 有权
    制备2-取代苯并呋喃-3-基硼酸酯的方法

    公开(公告)号:US08580976B2

    公开(公告)日:2013-11-12

    申请号:US13685209

    申请日:2012-11-26

    Abstract: The invention relates to a process for preparing a stable 2-substituted benzofuran-3-yl borate ester corresponding to the formula: said process comprising contacting 3-bromo-2-substituted-benzofuran corresponding to the formula: with an C1-4 alkyllithium at a temperature less than −60° C. to form 3-lithio-2-substititued-benzofuran, contacting the 3-lithio-2-substituted- benzofuran at a temperature less than −60° C. with an borate ester corresponding to the formula: and recovering the resulting borate ester product, wherein, RW' is C1-4 alkyl; Rx is C1-10 hydrocarbyl or halohydrocarbyl; and RY independently each occurrence is C1-10 hydrocarbyl, halohydrocarbyl or trialkylsilylhydrocarbyl or 2 RY groups together are a divalent hydrocarbylene of up to 20 carbons.

    Abstract translation: 本发明涉及一种制备对应于下式的稳定的2-取代的苯并呋喃-3-基硼酸酯的方法:所述方法包括使对应于下式的3-溴-2-取代的苯并呋喃与C1-4烷基锂接触 温度低于-60℃以形成3-亚硫基-2-取代的苯并呋喃,在低于-60℃的温度下将3-二硫-2-取代的苯并呋喃与对应于式 并回收得到的硼酸酯产物,其中,RW'为C 1-4烷基; Rx是C 1-10烃基或卤代烃基; 每个R 1独立地为C 1-10烃基,卤代烃基或三烷基甲硅烷基烃基或2个RY基团一起为至多20个碳原子的二价亚烃基。

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