Issue 4, 2020

Sulfur-directed palladium-catalyzed C(sp3)–H α-arylation of 3-pyrrolines: easy access to diverse polysubstituted pyrrolidines

Abstract

A sulfur-directed palladium-catalyzed C(sp3)–H α-arylation of 3-pyrrolines has been disclosed by installing a thioacyl group as the directing group. The arylation reactions using arylboronic acids as coupling partners provided a variety of 2-aryl-3-pyrolines in moderate to good yields. Moreover, the α-arylated products were readily converted to various synthetically useful 3-pyrroline and pyrrolidine derivatives, especially polysubstituted pyrrolidines.

Graphical abstract: Sulfur-directed palladium-catalyzed C(sp3)–H α-arylation of 3-pyrrolines: easy access to diverse polysubstituted pyrrolidines

Supplementary files

Article information

Article type
Research Article
Submitted
02 Dec 2019
Accepted
17 Jan 2020
First published
20 Jan 2020

Org. Chem. Front., 2020,7, 666-671

Sulfur-directed palladium-catalyzed C(sp3)–H α-arylation of 3-pyrrolines: easy access to diverse polysubstituted pyrrolidines

G. Sun, X. Zou, J. Wang and W. Yang, Org. Chem. Front., 2020, 7, 666 DOI: 10.1039/C9QO01440C

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