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Intramolecular Copper(I)-Catalyzed Interrupted Click/Acylation Domino Reaction.

08:00 EDT 12th July 2019 | BioPortfolio

Summary of "Intramolecular Copper(I)-Catalyzed Interrupted Click/Acylation Domino Reaction."

Acyl substituted triazoles are valuable scaffolds, but the direct synthesis of these moieties from terminal alkynes via copper catalysis remains unexplored. We report a robust, general and efficient method using a simple CuI/2,2'-bipyridine catalytic system. This transformation involves a copper catalyzed azide-alkyne cycloaddition (CuAAC) followed by an intramolecular acylation onto a carbamoyl chloride. The reaction proceeds under mild conditions, tolerates several functional groups and is readily scalable. This method represents a novel strategy towards the synthesis of complex heterocycles via a CuAAC/acylation domino process.

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This article was published in the following journal.

Name: Angewandte Chemie (International ed. in English)
ISSN: 1521-3773
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