Ruthenium(II)-Catalyzed Asymmetric Inert C-H Bond Activation Assisted by a Chiral Transient Directing Group
Ruthenium(II)-Catalyzed Asymmetric Inert C-H Bond Activation Assisted by a Chiral Transient Directing Group
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DOI：
10.1002/anie.201913733
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发表时间：
2020-01-23
影响因子：
16.6
通讯作者：
Wang, Jun
中科院分区：
文献类型：
--
作者：
Li, Guozhu;Liu, Qinzhe;Wang, Jun
研究了钌（II）催化的手性瞬时导向基团辅助的不对称分子内氢化反应。制备了一系列具有手性全碳季位立体中心的2,3-二氢苯并呋喃，其产率高达98%，对映选择性高达50% ~ 99%。通过这种方法，成功地开发了一种新的CB2受体激动剂MDA7的不对称全合成方法。
A ruthenium(II)-catalyzed asymmetric intramolecular hydroarylation assisted by a chiral transient directing group has been developed. A series of 2,3-dihydrobenzofurans bearing chiral all-carbon quaternary stereocenters have been prepared in remarkably high yields (up to 98 %) and enantioselectivities (up to >99 % ee). By this methodology, a novel asymmetric total synthesis of CB2 receptor agonist MDA7 has been successfully developed.