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Ruthenium(II)-Catalyzed Asymmetric Inert C-H Bond Activation Assisted by a Chiral Transient Directing Group.
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2019-12-23 , DOI: 10.1002/anie.201913733
Guozhu Li 1 , Qinzhe Liu 1 , Laxmaiah Vasamsetty 1 , Weicong Guo 1 , Jun Wang 1
Affiliation  

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.

中文翻译:

钌(II)催化的手性瞬态导向基团辅助的不对称惰性CH键活化。

已经开发了由手性瞬态导向基团辅助的钌(II)催化的不对称分子内氢芳基化反应。制备了一系列带有手性全碳四元立体中心的2,3-二氢苯并呋喃,具有很高的收率(高达98%)和对映选择性(高达> 99%ee)。通过这种方法,已经成功地开发了新颖的不对称的CB2受体激动剂MDA7的全合成。
更新日期:2020-01-23
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