ArticleACS medicinal chemistry letters2026
Synthesis of 1,3-Dihydro-2,1-benzisoxazoles by Intramolecular C-N Coupling: Evaluation as an Indane Bioisostere.
Article in ACS medicinal chemistry letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Despite the ever-increasing interest in isoxazole-based compounds, benzo-fused isoxazolidines, or 1,3-dihydro-2,1-benzisoxazoles, are very rare. Seeking to fill this gap, we present a method for the synthesis of 1,3-dihydro-2,1-benzisoxazoles by intramolecular Cu-mediated or Pd-catalyzed C-N coupling of bromoaryl benzylic hydroxylamine derivatives, which can be further derivatized through a simple reductive amination sequence. This approach overcomes the limitations of previous methods and provides access to multiple novel heterocyclic scaffolds. As a proof of concept, we apply the method to the synthesis of a benzisoxazoline analogue of the metabolically labile chiral indane-based MT1/MT2 receptor agonist ramelteon, ultimately furnishing a compound with a >10-fold improvement in metabolic stability in human hepatocytes. Support for the bioisosteric nature of the 1,3-dihydro-2,1-benzisoxazole and indane cores was provided in the context of the ramelteon analogue by DFT calculations.
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