Given the widespread presence of nitrogen-containing heterocycles in active pharmaceutical ingredients, methods for their synthesis are of paramount importance. Unfortunately, the nitrogen atoms that impart many of the beneficial properties of heterocycles adds an extra element of synthetic complexity when applying cross-coupling approaches for their incorporation, due to nonproductive binding to transition-metal catalysts. Thus, de novo methods for complex heterocycle synthesis are valuable. Herein we describe a conceptually different approach to access pyrrolo[2,3,b]pyridines (7-azaindoles) and imidazopyridines from the same amine starting materials.

Divergent heterocycle synthesis from primary amines using halomucononitriles

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ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.