Preparation of (Z)‑α,β-Disubstituted Enamides via Palladium-Catalyzed Addition of Boronic Acids to Ynamides

A Pd-catalyzed, highly regio- and stereoselective addition of boronic acids to ynamides has been realized. This protocol generates (Z)-α,β-disubstituted enamides in high yields with excellent regio- and stereoselectivity under the mild reaction conditions, thereby providing a good complementary method for the diverse synthesis of multifunctional enamides. A wide collection of functional groups are found to be tolerated. It represents a straightforward and useful means to assemble stereodefined enamides from readily available starting materials.

本研究成功实现了钯催化的硼酸与炔酰胺间的高区域及立体选择性加成反应。该反应体系在温和反应条件下，以优异的区域和立体选择性及较高收率生成(Z)-α,β-二取代烯酰胺，从而为多官能团化烯酰胺的多样化合成提供了优良的补充方法。该反应具有良好的官能团兼容性，代表了一种从易得起始原料出发，构建立体规整烯酰胺的简洁实用途径。