1. Ruthenium(II)‐katalysierter Late‐Stage Einbau von N‐Aryltriazolen und ‐tetrazolen mit Sulfoniumsalzen per C−H‐Aktivierung.
- Author
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Simon, Hendrik, Zangarelli, Agnese, Bauch, Tristan, and Ackermann, Lutz
- Subjects
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COUPLING reactions (Chemistry) , *OXIDATIVE addition , *AUTHOR-reader relationships , *TOLUENE , *OXAZOLINE - Abstract
This article discusses a study on the late-stage functionalization of pharmaceutical drugs using ruthenium-catalyzed C-H activation. The researchers focused on introducing N-Aryltriazoles and Tetrazoles into drug molecules, as these structures have the potential to enhance their activity. The method described in the article utilizes accessible dibenzothiophenium salts for the C-H arylation, allowing for the incorporation of these motifs into various bioactive compounds. The study demonstrates that the method is cost-effective, efficient, and compatible with complex dibenzothiophenium salts derived from pharmaceuticals and natural products. Mechanistic studies were conducted to understand the reaction mechanism, and the researchers proposed a catalytic cycle involving the formation of an active catalytic species. Overall, this study provides a mild and versatile method for the synthesis of medicinally relevant compounds. [Extracted from the article]
- Published
- 2024
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