Abstract

Herein, we report an efficient strategy towards the synthesis of amino acid substituted isoquinoline derivativesviareaction of unprotected amino acid/amino acid ester/amino acid based drugs with 2-(2-oxo-2-aryl/alkylethyl)benzonitrile under metal-free conditions. The developed protocol is highly simple and shows functional group tolerance to provide corresponding novel amino acid substituted isoquinolines in aqueous medium. The applicability of the reaction is an easier modification of well-known drugs and successfully extended to gram-scale synthesis.

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