对映选择性铜催化硼化环化反应合成喹唑啉酮。

Department of Chemistry, University of Manchester, Oxford Road, Manchester, M13 9PL, UK.

School of Material and Chemical Engineering, Xuzhou University of Technology, Xuzhou, 221018, P.R. China.

Angew Chem Int Ed Engl. 2021 Jun 21;60(26):14355-14359. doi: 10.1002/anie.202103259. Epub 2021 May 19.

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.

喹唑啉酮是具有重要药用价值的分子中的常见结构单元。我们报告了一种对映选择性铜催化的硼化环化反应，用于构建优先的吡咯并喹唑啉酮基序。该反应具有高对映选择性和非对映选择性控制，可以提供含有季立体中心的产物。通过进一步的操作证明了产物的实用性。