Sulfur‐Enabled Malonic Acid‐Assisted Facile Transformation of Arylacetonitriles/Acetonitriles to Primary Thioamides

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Abstract
Thioamide‐containing molecules represent a valuable class of candidates widely utilized in medicinal chemistry and hence have attracted great attention. Herein, we disclose an efficient protocol for the transformation of aryl and alkyl acetonitriles to their corresponding thioamides with elemental sulfur and malonic acid in the presence of a base. The developed protocol offers advantage of broader substrate scope and operates under operationally simple conditions, delivering high yield of products in just one hour. The observations from test experiments reveals malonic acid as hydrogen donor, and found essential for this thioamidation reaction. The gram‐scale synthesis demonstrates the scalability of the method, whereas further synthetic transformation highlights synthetic potentials of derivatives.

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