Facile Synthesis of Tetrahydro-1<i>H</i>-isoindolones via a Sequential Three-Component Copper-Catalyzed Coupling/Propargyl-Allenyl Isomerization/[4 + 2] Cyclization Reaction

An interesting sequential three-component copper-catalyzed coupling/propargyl-allenyl isomerization/[4 + 2] cyclization reaction, providing a facile synthesis of highly substituted tetrahydro-1H-isoindolones from conjugated vinylic alkynes, imines, and α,β-unsaturated enoic acid chlorides is reported. The most attractive feature of this transformation is that three stereogenic centers could be generated in one step with high diastereoselectivity.本研究报道了一种颇具研究价值的连续三组分铜催化偶联/炔丙基-联烯异构化/[4+2]环化反应，该反应可通过共轭烯炔、亚胺与α,β-不饱和烯酰氯的原料体系，便捷合成高度取代的四氢-1H-异吲哚啉酮。该转化最引人关注的特点在于，可一步构建三个手性中心，且具备优异的非对映选择性。