Me3Al mediated domino nucleophilic addition/intramolecular cyclisation of 2-(2-oxo-2-phenylethyl)benzonitriles with amines; A convenient approach for the synthesis of substituted 1-aminoisoquinolines

Submitting author affiliation:
City University of New York, new york, United States

Beilstein Arch. 2021, 202126.

Published 22 Mar 2021



A simple and efficient protocol for the construction of 1-aminoisoquinolines was achieved by treating 2-(2-oxo-2-phenylethyl)benzonitriles with amines in the presence of Me3Al. The reaction proceeds via a domino nucleophilic addition with subsequent intramolecular cyclisation. This method provides wide variety of substituted 1-aminoisoquinolines with good functional group tolerance. Furthermore, the synthetic utility of this protocol was demonstrated in the successful synthesis of antitumor agent CWJ-a-5 in gram scale.

Keywords: 1-aminoisoquinolines CWJ-a-5 2-(2-oxo-2-phenylethyl)benzonitriles nucleophilic addition intramolecular cyclisation

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Adusumalli, M. S. K.; Konidena, L. N. S.; Gandham, H. B.; Kumari, K.; Valluru, K. R.; Nidasanametla, S. K. R.; Battula, V. R.; Namballa, H. K. Beilstein Arch. 2021, 202126. doi:10.3762/bxiv.2021.26.v1

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