Synthesis of Novel 4-Fluoro-2H-pyrazol-3-ylamines

Abstract

A new and efficient synthesis for the preparation of novel 4-fluoro-2H-pyrazol-3-ylamines is described. It involves the reaction of an acyl chloride with fluoroacetonitrile and sequential ring closure of the α-fluoro-β-ketonitrile with hydrazine. Utilizing this synthetic protocol, we have synthesized a variety of 4-fluoro-2H-pyrazol-3-ylamines with different steric and electronic demands.

Keywords:

• Aminopyrazole
• fluoro
• 4-fluoro-2H-pyrazol-3-ylamines

Notes

^a Evaluated by LCMS of the crude solution.