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Updated: Jul 28, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Nitrogen Atom Transfer Enables the (5+1) Annulation Reaction to Access Aminoisoquinolines
Gayyur1, Shivani Choudhary1,2, Ruchir Kant3
1Medicinal & Process Chemistry Division and CSIR-Central Drug Research Institute, Lucknow 226031, U.P., India.
Abstract:
Herein, a catalytic synthetic transformation offering a series of -NH2 group-bearing aminoisoquinolines with moderate to good yields has been showcased. Interestingly, the nitrogen atom of the isoquinoline ring is coming from the reaction medium upon metal-assisted C≡N bond cleavage. Moreover, this (5+1) annulation reaction shows broad substrate variation. Furthermore, the derivatization of the isoquinoline core via functional group interconversions and mechanistic studies to identify the reaction intermediate have been carried out successfully.
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