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Direct Preparation of N-Substituted Pyrazoles from Primary Aliphatic or Aromatic Amines.


ABSTRACT: Despite a large number of synthesis procedures for pyrazoles known today, those directly employing primary amines as substrates are rare. Herein, we report an original method for the preparation of N-alkyl and N-aryl pyrazoles from primary aliphatic or aromatic amines as a limiting reagent of the reaction. The protocol utilizes no inorganic reagents and requires a short reaction time, mild conditions, and the use of structurally simple and commercially available starting reagents. During this study, pyrazoles containing a wide variety of N-substituents were obtained using the same procedure for both aliphatic and aromatic amines.

SUBMITTER: Gulia N 

PROVIDER: S-EPMC8389898 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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Direct Preparation of <i>N</i>-Substituted Pyrazoles from Primary Aliphatic or Aromatic Amines.

Gulia Nurbey N   Małecki Marcin M   Szafert Sławomir S  

The Journal of organic chemistry 20210701 14


Despite a large number of synthesis procedures for pyrazoles known today, those directly employing primary amines as substrates are rare. Herein, we report an original method for the preparation of <i>N</i>-alkyl and <i>N</i>-aryl pyrazoles from primary aliphatic or aromatic amines as a limiting reagent of the reaction. The protocol utilizes no inorganic reagents and requires a short reaction time, mild conditions, and the use of structurally simple and commercially available starting reagents.  ...[more]

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