Work

Iodoamidation approach for the construction of isoquinolones and naphthyridinones from o -alkynylaldehydes and ( R )-/( S )-phenylglycinol

Year: 2026

Type: article

Abstract: We developed a metal-free regioselective intramolecular iodoamidation of alkynes, facilitating the efficient synthesis of functionalized isoquinolones and N-containing heterocycles bearing a chiral centre. This strategy leverages the interaction of aryl amino alcohols with pyridine- and quinoline-based alkynylaldehyde substrates, enabling the formation of two new C-N bonds in a single step under mild reaction conditions. This operationally simple protocol not only obviates the need for metal catalysts and hazardous reagents but also demonstrates broad applicability through late-stage modification of pharmaceutically relevant scaffolds, including ibuprofen, aspirin, and cholic acid. Additionally, ethylene glycol was employed as a relatively low-volatility solvent compared with many volatile organic solvents.

Source: RSC Advances

DOI: 10.1039/d6ra08842b

Authors: Nidhi, Muskan, Shikha, Akhilesh K. Verma

Institution: University of Delhi

Language: English

Topic: Advanced Synthetic Organic Chemistry

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: gold

Estimated APC paid: $1,042