We have developed a mild and scalable catalyst-free [3 + 2] cyclization of dihydroisoquinolines and isatin-derived Morita–Baylis–Hillman carbonates. The incorporation of tetrahydroisoquinoline and spirooxindole frameworks could be realized affording highly functionalized heterocycles in moderate to excellent yields with good diastereocontrols (up to 92% yields, >20 : 1 dr). The extension of this method
我们已经开发出温和且无可扩展性的二氢
异喹啉和
靛红衍生的森田-贝利斯-希尔曼
碳酸盐的无催化剂[3 + 2]环化反应。可以实现
四氢异喹啉和螺氧杂
吲哚骨架的结合,以中等至优异的产率提供高度官能化的杂环,并具有良好的非对映异构控制(高达92%的产率,> 20:1 dr)。该方法已扩展到二氢-β-咔啉。克级反应可以成功进行,从而有可能在进一步的
生物医学研究中应用。