Regioselective synthesis of N1-substituted-4-nitropyrazole-5-carboxylates via the cyclocondensation of ethyl 4-(dimethylamino)-3-nitro-2-oxobut-3-enoate with substituted hydrazines

Org Biomol Chem. 2022 Dec 14;20(48):9746-9752. doi: 10.1039/d2ob02006h.

Abstract

A simple and expeditious method for the regioselective synthesis of N1-substituted-4-nitropyrazole-5-carboxylates was developed. The method involves cyclocondensation of ethyl 4-(dimethylamino)-3-nitro-2-oxobut-3-enoate with a series of monosubstituted hydrazines to give N1-substituted-4-nitropyrazole-5-carboxylates with excellent regioselectivity and good yields. Solvent effects on regioselectivity of the cyclocondensation were examined.

MeSH terms

  • Carboxylic Acids*
  • Cyclization
  • Hydrazines*

Substances

  • Hydrazines
  • Carboxylic Acids