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Copper Catalyzed Asymmetric Dearomative Alkynylation of Isoquinolines

Abstract

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

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Article information


Submitted
09 Jan 2020
Accepted
08 Feb 2020
First published
11 Feb 2020

Org. Chem. Front., 2020, Accepted Manuscript
Article type
Research Article

Copper Catalyzed Asymmetric Dearomative Alkynylation of Isoquinolines

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

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