An Efficient Nickel-Catalyzed Asymmetric Oxazole-Forming Ugi-Type Reaction for the Synthesis of Chiral Aryl-Substituted THIQ Rings
An Efficient Nickel-Catalyzed Asymmetric Oxazole-Forming Ugi-Type Reaction for the Synthesis of Chiral Aryl-Substituted THIQ Rings
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用于合成手性芳基取代的 THIQ 环的高效镍催化不对称恶唑形成 Ugi 型反应
DOI：
10.1002/chem.201700970
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发表时间：
2017
影响因子：
4.3
通讯作者：
Wang Rui
中科院分区：
文献类型：
--
作者：
Li Dan;Yang Dongxu;Wang Linqing;Liu Xihong;Wang Kezhou;Wang Jie;Wang Pengxin;Liu Yuyang;Zhu Haiyong;Wang Rui
本发明公开了一种镍催化的C，N-环甲亚胺和异腈的不对称恶唑生成UGI反应。报道的方案进展顺利，并通过使用容易获得的手性二胺作为配体，以良好的产率和良好的对映选择性给出了相应的加合物，其中包含两个重要的药物活性环系(四氢喹啉和恶唑环)。这一简单而有效的策略提供了一系列C1取代的芳基四氢异喹啉的容易获得的途径。
A nickel‐catalyzed asymmetric oxazole‐forming Ugi reaction of C,N‐cyclic azomethine imines and isonitriles is disclosed. The reported protocol proceeds smoothly, and gives the corresponding adducts, which contain two important pharmaceutically active ring‐systems (tetrahydroquinoline and oxazole rings), in good yields and excellent enantioselectivities by employing an easily accessible chiral diamine as a ligand. This simple and efficient strategy provides easy access to a series of C1‐substituted aryl tetrahydroisoquinolines.