Palladium-Catalyzed Cross-Coupling of Aryl Bromides and Chlorides with Trimethylsilylalkynes under Mild Conditions
Adrian Tlahuext-Aca1, Quyen D Nguyen1, Yang Gao1
1Corteva Agriscience, Small Molecule Discovery and Development, Indianapolis, Indiana 46268, United States.
Abstract:
Herein, we disclose a palladium-catalyzed cross-coupling of aryl bromides and chlorides with trimethylsilylalkynes under mild reaction conditions. This method utilizes commercially available and air stable palladium precatalysts and avoids the use of copper cocatalysts. Moreover, it allows for the synthesis of a wide range of disubstituted alkynes in high yields with excellent functional group tolerance. The utility of the developed method was further demonstrated via the late-stage alkynylation of pharmaceuticals and natural bioactive compounds.
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