Construction of 3-Hydroxyindolin-2-ones via Ru(II)-Catalyzed Domino Alkylation/Cyclization/Oxidation of 2-Aminophenethanols

Organic Letters, Journal Year: 2025, Volume and Issue: unknown

Published: April 24, 2025

A novel Ru(II)-catalyzed domino reaction, comprising alkylation, cyclization, and oxidation of 2-aminophenethanols with benzyl alcohols, has been developed for the synthesis 3-hydroxyindolin-2-ones. This transformation exhibits excellent synthetic efficiency, enabling selective formation four or three σ bonds, one π bond, quaternary carbon center in step under identical conditions. Furthermore, it provides a versatile approach to 3-hydroxyindolin-2-one frameworks distinct substituents at 1- 3-positions.

Language: Английский

Late-Stage N-Arylation of Tryptophan-Containing Peptides and Drug Molecules via Arylthianthrenium Salts

Organic Letters, Journal Year: 2025, Volume and Issue: unknown

Published: May 15, 2025

We report herein a mild and efficient method for the late-stage N-arylation of tryptophan tryptophan-containing peptides using readily accessible arylthianthrenium salts through dual photoredox/copper catalysis. Applying this protocol, library noncanonical amino acids N-arylated was facilely prepared. Moreover, protocol enables peptide ligation conjugation, offering convenient access to ligated peptide/drug conjugates. Remarkably, strategy can also be applied modification complex drug molecules.

Language: Английский