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    Arylation method for the functionalization of O-allyl erythromycin derivatives
    8.
    发明授权
    Arylation method for the functionalization of O-allyl erythromycin derivatives 有权
    O-烯丙基红霉素衍生物官能化的酰化方法

    公开(公告)号：US07071314B2

    公开(公告)日：2006-07-04

    申请号：US10156404

    申请日：2002-05-28

    申请人： Weijang Zhang ,  Margaret Chi-Ping Hsu ,  Anthony R. Haight ,  Matthew John Peterson ,  Bikshandarkoil A. Narayanan

    发明人： Weijang Zhang ,  Margaret Chi-Ping Hsu ,  Anthony R. Haight ,  Matthew John Peterson ,  Bikshandarkoil A. Narayanan

    IPC分类号： C07H1/00

    CPC分类号： C07H17/08

    摘要： An efficient arylation technique for use in the synthesis of erythromycin derivatives, involving a modified Heck reaction which employs less than six mole percent of palladium catalyst and no phosphine is disclosed. With this modified Heck reaction, an O-alkenylaryl macrolide can be obtained in a much shorter reaction time than under conventional Heck reaction conditions. The modified Heck reaction can be utilized in a method for phosphine-free arylation of an O-allylic erythromycin derivative, in a method for preparing an O-alkenylaryl erythromycin A derivative, or in a method for preparing a 2′, 4″-hydroxyl protected 6-O-alkenylaryl erythromycin A derivative.

    摘要翻译： 公开了一种用于合成红霉素衍生物的有效芳基化技术，涉及使用少于6摩尔％钯催化剂和不含膦的改性Heck反应。 通过该改进的Heck反应，可以在比常规Heck反应条件下短得多的反应时间内获得O-链烯基芳基大环内酯。 改性的Heck反应可用于O-烯丙基红霉素A衍生物的制备方法中的O-烯丙基红霉素衍生物的无磷化氢芳基化方法，或者用于制备2'，4“ 羟基保护的6-O-链烯基芳基红霉素A衍生物。