We report the first demonstrations of intra- and intermolecular acyclic nitronate olefin cycloaddition (ANOC) reactions that enable the highly efficient syntheses of isoxazolines bearing various functional groups. This general approach...

In this work, the green esterification of carboxylic acids promoted by tert‐butyl nitrite has been well developed. This transformation is compatible with a broad range of substrates and exhibits excellent functional group tolerance. Various drugs and substituted amino acids are applicable to this reaction under near neutral conditions, with good to excellent yields.

Herein, we report a molecular iodine‐catalysed reductive alkylation of indoles with carbonyl compounds using Et3SiH for the efficient synthesis of C3‐alkylated indoles. This metal‐free and environmental‐friendly process exhibits excellent functional group tolerance, mild conditions, and wide substrate scope. Notably, the synthetic usefulness of this strategy to pharmacochemistry was highlighted by the late‐stage modification of drug‐like molecules.

N-Tosylhydrazones have proven to be versatile synthons over the past several decades. However, to our knowledge, the construction of isoxazolines based on N-tosylhydrazones has not been examined. Herein, we report...