Enantioselective synthesis of cyclic α-aminoboronates <i>via</i> copper-catalyzed dearomative borylation of 4-quinolinols
作者:Ming Xu、Yizhao Ouyang、Linghua Wang、Shuai Zhang、Pengfei Li
DOI:10.1039/d2cc00027j
日期:——
using a Cu(I)/(R,R)-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.
使用 Cu( I )/( R , R )-Ph-BPE 催化剂开发了 4-喹啉醇的高度对映选择性和区域选择性去芳基化硼酸化,用于高效合成前所未有的杂环 α-氨基硼酸盐,一类可能与药物相关的新型化合物发现,通常具有优异的产率和对映选择性。该产品也是高度官能化的四氢喹啉和环状α-氨基硼酸酯衍生物的有用中间体。