Palladium-Catalyzed Construction of Trisubstituted Oxazoles from Trifluoroalanine Derivatives

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.