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Enantioselective Copper-Catalyzed Borylative Cyclization for the Synthesis of Quinazolinones.


ABSTRACT: 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.

SUBMITTER: Dherbassy Q 

PROVIDER: S-EPMC8252434 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature

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Enantioselective Copper-Catalyzed Borylative Cyclization for the Synthesis of Quinazolinones.

Dherbassy Quentin Q   Manna Srimanta S   Shi Chunling C   Prasitwatcharakorn Watcharapon W   Crisenza Giacomo E M GEM   Perry Gregory J P GJP   Procter David J DJ  

Angewandte Chemie (International ed. in English) 20210519 26


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. ...[more]

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