Issue 49, 2016

A palladium-catalyzed intramolecular carbonylative annulation reaction for the synthesis of 4,5-fused tricyclic 2-quinolones

Abstract

A concise and efficient synthetic route to 4,5-fused tricyclic 2-quinolones through the palladium-catalyzed carbonylative annulation of alkyne-tethered N-substituted o-iodoanilines has been developed. This reaction proceeds smoothly under mild reaction conditions and exhibits exceptional tolerance to a variety of functional groups. It has been successfully applied to the efficient synthesis of BI 224436, an HIV integrase inhibitor.

Graphical abstract: A palladium-catalyzed intramolecular carbonylative annulation reaction for the synthesis of 4,5-fused tricyclic 2-quinolones

Supplementary files

Article information

Article type
Communication
Submitted
27 Mar 2016
Accepted
19 May 2016
First published
19 May 2016

Chem. Commun., 2016,52, 7665-7667

A palladium-catalyzed intramolecular carbonylative annulation reaction for the synthesis of 4,5-fused tricyclic 2-quinolones

X. Zhang, H. Liu and Y. Jia, Chem. Commun., 2016, 52, 7665 DOI: 10.1039/C6CC02600A

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