Patent · US Active

Asymmetrically catalyzed synthesis method of nitropyrazole amide compound

US10464899B2 · kind B2 · utility

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15Claims
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Inventors

Key dates

Filing dateJun 12, 2015
Grant dateNov 5, 2019
Priority date
Expiry dateAug 23, 2035

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D409/06
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A synthesis method of γ-nitropyrazole amide compound through asymmetrical catalyzing technique is provided, a nitroalkane and an α,β-unsaturated pyrazole amide are applied as the raw material, a complex formed by a chiral amine oxide with a rare earth metal compound is served as the catalyst, a 4 Å molecular sieve is served as an additive, the γ-nitropyrazole amide compound can be obtained with a yield more than 99% and enantiomeric excess more than 99% ee. The catalytic system not only has the advantages of simple operation, mild reaction conditions, requiring no acid/base additives, convenient product purification, high yield and enatioselectivity, compliance with green atomic economy, and promising prospects for industrial application, but also allows the obtained γ-nitropyrazole amide compound to undergo some simple chemical conversions to produce some molecules having physiological activities.

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