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Published on: August 12, 2019
TFA-catalyzed solvent-free dearomative cyanidation of isoquinoline using (Boc)2O as an acylation agent
Xujin Zhang1,2, Lihua Huang1,2, Ye Zhang1,2
1School of Chemical Engineering, Sichuan University of Science & Engineering, Zigong, Sichuan 643000, P. R. China. pharmaceutics@163.com.
Abstract:
A TFA-catalyzed dearomative cyanidation of isoquinoline is described, which provides a series of 1-cyanoisoquinolines in high yields under solvent-free conditions. This protocol is operated under mild and environmentally friendly conditions, utilizing readily available and cost-effective starting materials. The reaction features broad functional group compatibility, 100 mmol scale synthesis ability and operational simplicity, making it a significant potential approach for the synthesis of various biologically interesting isoquinolines via α C-cyanation.
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