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MINI REVIEW article

Front. Chem.

Sec. Medicinal and Pharmaceutical Chemistry

Volume 13 - 2025 | doi: 10.3389/fchem.2025.1553975

This article is part of the Research Topic Quinoline as Lead Structures for the Development of Leishmanicidal Agents View all 3 articles

4-Aminoquinoline: A Comprehensive Review about Synthetic Strategies

Provisionally accepted
  • 1 Universidad de la República, Montevideo, Uruguay
  • 2 Pasteur Institute of Montevideo, Montevideo, Uruguay
  • 3 Central University of Venezuela, Caracas, Venezuela

The final, formatted version of the article will be published soon.

    4-Aminoquinoline represents an important scaffold by their variety of applications in medicinal chemistry, synthetic organic and industrial chemistry. It has gained great relevance for the development of selective and potent leishmanicidal agents targeting parasite mitochondria, agonist and antagonist of TLRs, antimalarials and anticancer agents. Then, as consequence of the importance of the 4-aminoquinoline as leishmanicidal, the present mini-review article aims to give a comprehensive information about the different synthetic alternative for the synthesis of 4aminoquinolines including: (i) reactions based on nucleophilic aromatic substitution via conventional heating, microwave and ultrasound; (ii) one-pot reactions of inter-and intramolecular cyclization/annulation free metal or metal-catalyzed; (iii) miscellaneous reactions including dehydrogenative amination of dihydroquinolin-4(1H)one, amination via Hartwig-Buchwald crosscoupling or rearrangement reactions.

    Keywords: 4-Aminoquinoline, 4, 7-dichloroquinoline, SNAr, annulation

    Received: 31 Dec 2024; Accepted: 05 Mar 2025.

    Copyright: © 2025 Romero, Delgado, Benítez and Gotopo. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

    * Correspondence: Angel Romero, Universidad de la República, Montevideo, Uruguay

    Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.

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