Catalytic system-controlled divergent reactions of pyrazolidinones with 3-alkynyl-3-hydroxyisoindolinones to construct diversified nitrogen-containing heterocyclic scaffolds

TL;DR

Scientists developed a new catalytic method to create diverse nitrogen-based ring structures useful in drug discovery.

Contribution

This is the first method to use pyrazolidinones and propargyl alcohols to form tetrahydropyrimidinones and 3-acylindoles via selective N–N bond activation.

Findings

A catalytic system enabled the formation of three distinct nitrogen-containing heterocycles.

The method uses readily available starting materials and achieves moderate to good yields.

The process involves selective N–N bond activation and annulation cascade for scaffold construction.

Abstract

A catalytic system-controlled divergent reaction was reported to construct three distinct nitrogen-containing heterocycles from readily available starting materials via a precise chemical bond activation and annulation cascade. Notably, this is the first capture of pyrazolidinones and propargyl alcohols to construct tetrahydropyrimidinones via selective N–N bond activation and to generate previously unreported 3-acylindoles. This protocol demonstrates a broad substrate scope, moderate to good yields, and valuable transformations, laying a robust foundation for drug discovery applications.

A catalytic system-controlled divergent reaction was reported to construct three distinct nitrogen-containing heterocycles from readily available starting materials via a precise chemical bond activation and annulation cascade.

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