Reacción #8527

ord-3aa39437285a4e61ad16bed02546d92a

Ecuación de reacción

[H][H]
hydrogen
Nc1ccc(F)c(F)c1F
2,3,4-Trifluoroaniline
COC(=O)C(C)=O
methyl pyruvate
O=S(=O)([O-])[O-].[Mg+2]
magnesium sulfate
COC(=O)C(C)Nc1ccc(F)c(F)c1F
title compound
Rendimiento 95.3%
COC(=O)C(C)Nc1ccc(F)c(F)c1F
Methyl 2-(2,3,4-trifluoroanilino)propionate
Rendimiento 95.3%

Disolventes

Condiciones de reacción

Condiciones detalladas
See reaction.notes.procedure_details.

Tratamiento posterior

  1. 1
    FiltraciónAfter filtering off Pd—C and magnesium sulfate
  2. 2
    Concentraciónthe obtained filtrate was concentrated under reduced pressure
  3. 3
    OtroThe crystals thus precipitated
  4. 4
    Filtraciónwere filtered
  5. 5
    Lavadowhile washing with hexane

Procedimiento

2,3,4-Trifluoroaniline (2.94 g) and methyl pyruvate (2.04 g) were dissolved in methanol (30 ml). After adding 5% Pd—C (2.0 g) and anhydrous magnesium sulfate (2.65 g), the mixture was stirred at 50° C. in a hydrogen atmosphere for 16 hours. After filtering off Pd—C and magnesium sulfate, the obtained filtrate was concentrated under reduced pressure. The crystals thus precipitated were filtered while washing with hexane. Thus the title compound (4.44 g) was obtained as slightly yellowish crystals. Various spectral data of this product was identical with those obtained in Example 5.

Fuente

DOI: 10.6084/m9.figshare.5104873.v1Patente: US07087778B2uspto-grants-2006_08