Synthesis 2024; 56(20): 3131-3141
DOI: 10.1055/a-2368-8500
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Lewis Acid Mediated Synthesis of 4-Aminoquinoline Derivatives from 2-Aminobenzonitriles and Activated Alkynes via Aza-Michael and Annulation Reactions

Bikoshita Porashar
,
Anil K. Saikia
The authors are grateful to the Science and Engineering Research Board (SERB), New Delhi (Grant No. CRG/2022/001028) for financial support.


Abstract

An efficient methodology for the synthesis of highly diverse 4-aminoquinoline derivatives from activated alkynes and 2-aminobenzonitriles mediated by Lewis acid is described. The reaction proceeds via sequential aza-Michael addition/intramolecular annulation to afford highly substituted 4-aminoquinolines in good yields. The reaction is operationally simple and has high atom-economy with broad substrate scope. The post synthetic application of the reaction provides 4H-benzo[de][1,6]naphthyridines.

Supporting Information



Publication History

Received: 11 June 2024

Accepted after revision: 17 July 2024

Accepted Manuscript online:
18 July 2024

Article published online:
08 August 2024

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