Pd-Catalyzed Coupling of Aryl Chloride, Isocyanides, and Thiocarboxylate To Synthesize Thioamides.

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Tác giả: Zeyuan Fu, Liangbin Huang, Bingjie Rong

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: United States : Organic letters , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 722953

Although aryl chlorides are among the most abundant and stable aromatic electrophiles, the coupling of aryl chlorides with isocyanides has remained an unsolved challenge. Herein, we report a general transformation of aryl chlorides, isocyanides, and thiocarboxylates to synthesize thioamides. The sterically hindered and electron-rich Josiphos ligand significantly facilitates the rate-determining oxidative addition step and reduces the toxicity of isocyanides toward the metal center. The combination of thiocarboxylate as the nucleophile and Josiphos as the ligands enabled the coupling-tolerated various 1°, 2°, and 3° isocyanides, which provides a rapid, efficient, and versatile method for the synthesis of large quantities of thioamides, including those of pharmaceutical relevance.
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