Laccase-mediated chemoselective C-4 arylation of 5-aminopyrazoles.
basic_science · Level V
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- Record sourced from PubMed, PMID 39292681.
- Also identified by DOI 10.1371/journal.pone.0308036 and PMC identifier 11410246.
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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.
Medical subject headings
- Laccase
- Pyrazoles