Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 60, Issue 26, Pages 14355-14359Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202103259
Keywords
asymmetric; boron; copper; cyclization; nitrogen-containing heterocycles
Categories
Funding
- Leverhulme Trust (PDRA) [RPG-2016-360]
- European Union Horizon 2020 (Marie Sklodowska-Curie grant) [798846-CuCAN]
- Royal Government of Thailand (DPST scholarship)
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In this study, an enantioselective copper-catalyzed borylative cyclization was reported for the assembly of privileged pyrroloquinazolinone motifs. The reaction demonstrated high enantio- and diastereocontrol, yielding products with quaternary stereocenters. The utility of the products was further demonstrated through additional manipulations.
Quinazolinones are common substructures in molecules of medicinal importance. We report an enantioselective copper-catalyzed borylative cyclization for the assembly of privileged pyrroloquinazolinone motifs. The reaction proceeds with high enantio- and diastereocontrol, and can deliver products containing quaternary stereocenters. The utility of the products is demonstrated through further manipulations.
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