Xu Ming, Ouyang Yizhao, Wang Linghua, Zhang Shuai, Li Pengfei
Frontier Institute of Science and Technology, Xi'an Jiaotong University, 99 Yanxiang Road, Xi'an 710054, China.
State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China.
Chem Commun (Camb). 2022 Mar 15;58(22):3677-3680. doi: 10.1039/d2cc00027j.
A highly enantioselective and regioselective dearomative borylation of 4-quinolinols was developed using a Cu(I)/(,)-Ph-BPE catalyst for efficient synthesis of unprecedented heterocyclic α-amino boronates, a new class of compounds potentially relevant to drug discovery, in generally excellent yields and enantioselectivities. The products were also useful intermediates for highly functionalized tetrahydroquinolines and cyclic α-aminoboronate derivatives.
利用Cu(I)/(,)-Ph-BPE催化剂，开发了一种4-喹啉醇的高度对映选择性和区域选择性去芳构化硼化反应，用于高效合成前所未有的杂环α-氨基硼酸酯，这是一类可能与药物发现相关的新型化合物，产率和对映选择性通常都非常优异。这些产物也是用于高度官能化四氢喹啉和环状α-氨基硼酸酯衍生物的有用中间体。
