Enantioselective synthesis of cyclic α-aminoboronates via copper-catalyzed dearomative borylation of 4-quinolinols†
Shuai
Zhang 
a
and
Pengfei
Li
*ab
a
and
Pengfei
Li
*ab
Abstract
A highly enantioselective and regioselective dearomative borylation of 4-quinolinols was developed 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.
- This article is part of the themed collection: Boron Chemistry in the 21st Century: From Synthetic Curiosities to Functional Molecules
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