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Updated: Sep 18, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Palladium-Catalyzed Construction of Trisubstituted Oxazoles from Trifluoroalanine Derivatives
Junrui Wang1, Chuangchuang Liu1, Wenjie Ju1
1Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, P. R. China.
Abstract:
The preparation of trisubstituted oxazole rings, which serve as privileged structural motifs in bioactive molecules and natural products, presents synthetic challenges such as low efficiency and multistep procedures. Herein, we present a streamlined synthetic strategy enabling the one-step construction of trisubstituted oxazoles through a palladium-catalyzed Suzuki-Miyaura cross-coupling reaction. This practical protocol facilitates gram-scale synthesis while also enabling the direct preparation of the bioactive molecule Almazole D, highlighting its synthetic utility and importance.
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