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Synlett
DOI: 10.1055/a-2818-3037
DOI: 10.1055/a-2818-3037
Letter
Brønsted Acid-Mediated Synthesis of Isocoumarins and Isoquinolines
Autor*innen
We would like to thank financial support from the Natural Science Foundation of Gansu Province (No: 23JRRA1174) and the Gansu Provincial Innovation Fund for University Teachers (2025A-165) for their financial support.
Gefördert durch: Gansu Provincial Innovation Fund for University Teachers 2025A-165
Abstract
Heterocyclic compounds are of significant importance in the fields of organic synthesis and medicinal chemistry. Current synthetic methods for these molecules often rely on specific building blocks or transition-metal catalysis, which impose certain limitations in terms of methodology. Consequently, the development of metal-free synthetic methodologies for heterocycles is of great importance. In this study, readily available and inexpensive additives, TsOH·H₂O and CH₃COOH, were employed as the mediators. By modulating the solvent system, isocoumarin and isoquinoline derivatives were efficiently synthesized in CH₃CN and DMF, respectively. Notably, this method enables a rapid and efficient synthesis of the natural product Thunberginol A under metal-free conditions. This strategy offers a practical and efficient approach for constructing relevant drug-like core skeletons.
Publikationsverlauf
Eingereicht: 19. Januar 2026
Angenommen nach Revision: 19. Februar 2026
Artikel online veröffentlicht:
05. März 2026
© 2026. Thieme. All rights reserved.
Georg Thieme Verlag KG
Oswald-Hesse-Straße 50, 70469 Stuttgart, Germany
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