Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 59, Issue 9, Pages 3475-3479Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201913733
Keywords
asymmetric catalysis; CB2 receptor agonist; C-H activation; benzofurans; ruthenium(II)
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Funding
- National Natural Science Foundation of China [21971263, 21402244]
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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.
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