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Updated: May 23, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Enantioselective synthesis of bio-relevant 3,5-diaryl pyrazolines
Olivier Mahé1, Isabelle Dez, Vincent Levacher
1INSA de Rouen, St Etienne du Rouvray, France.
Abstract:
The straightforward asymmetric construction of bio-relevant Δ(2)-pyrazolines having either N-(thio)amide or N-acetyl functional groups and flanked by aryl substituents such as phenol at C3 and C5 has been achieved through an enantioselective phase transfer organocatalytic addition of N-Boc hydrazine to chalcones followed by a transprotection sequence allowing N-Boc transformation into N-CXNHR (X = S, O) or N-Ac functional groups. This approach was applied to a straightforward elaboration of chiral monoamine oxidase inhibitor derivatives.
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