Issue 6, 2020

Copper-catalyzed asymmetric dearomative alkynylation of isoquinolines

Abstract

Cu/(Ph-pybox)-catalyzed asymmetric dearomative alkynylation of isoquinolines has been realized in high to excellent enantioselectivities (up to 96% ee) with α-bromoacetophenone as an activator and 1,1′-binaphthyl-2,2′-diyl hydrogenphosphate as an additive. This novel reaction tolerates a wide variety of functional groups and affords enantioenriched C1-alkynyl 1,2-dihydroisoquinolines in high yields and ee under mild conditions.

Graphical abstract: Copper-catalyzed asymmetric dearomative alkynylation of isoquinolines

Supplementary files

Article information

Article type
Research Article
Submitted
09 Jan 2020
Accepted
08 Feb 2020
First published
11 Feb 2020

Org. Chem. Front., 2020,7, 829-833

Copper-catalyzed asymmetric dearomative alkynylation of isoquinolines

X. Kou, Q. Zhao and Z. Guan, Org. Chem. Front., 2020, 7, 829 DOI: 10.1039/D0QO00041H

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