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Updated: Jun 12, 2025

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Laccase-mediated chemoselective C-4 arylation of 5-aminopyrazoles
Mansour Shahedi1, Rojina Shahani1, Niloofar Omidi1
1Department of Organic Chemistry, Shahid Beheshti University, Tehran, Iran.
Abstract:
Chemoselective arylation of 5-aminopyrazoles was performed through oxidative formation of orthoquinones from catechols catalyzed by Myceliophthora thermophila laccase (Novozym 51003), and subsequently nucleophilic attack of 5-aminopyrazole to the catechol intermediates. The C-4 arylated products were obtained under extremely mild conditions without the need for amine protection or halogenation of the substrates. From this method, 10 derivatives with moderate to good efficiency (42-94%) were prepared.
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