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Ruthenium(II)‐Catalyzed Asymmetric Inert C−H Bond Activation Assisted by a Chiral Transient Directing Group
Author(s) -
Li Guozhu,
Liu Qinzhe,
Vasamsetty Laxmaiah,
Guo Weicong,
Wang Jun
Publication year - 2020
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201913733
Subject(s) - stereocenter , ruthenium , chemistry , intramolecular force , catalysis , enantioselective synthesis , medicinal chemistry , combinatorial chemistry , stereochemistry , organic chemistry
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.