Реакция #8326

ord-f20cb3d9c17f4dcbbbca7c8f90a35e53

Растворители

Условия реакции

Подробные условия
See reaction.notes.procedure_details.

Обработка

  1. 1
    workup.STIRRINGthe resulting mixture is stirred for 1 h
  2. 2
    КонцентрированиеThe mixture is concentrated in vacuo
  3. 3
    Другоеthe residue chromatographed on a SiO2 column (30% ethyl acetate/hexanes)

Методика

Boron trifluoride etherate (0.25 mL, 1.98 mmol) is added to a solution of 2-(4-fluoro-phenyl)-1-(6-methyl-pyridin-2-yl)-ethanone (0.45 g, 1.98 mmol) in tetrahydrofuran (6.6 mL) under nitrogen and stirred for 30 min. A solution of (R)-1-amino-5-benzyloxymethyl-pyrrolidin-2-one (0.43 g, 1.98 mmol) in tetrahydrofuran (1.0 mL) is added and the resulting mixture is stirred for 1 h. The mixture is concentrated in vacuo and the residue chromatographed on a SiO2 column (30% ethyl acetate/hexanes) to yield the title compound, 380 mg (45%), as a yellow foam.

Источник

DOI: 10.6084/m9.figshare.5104873.v1Патент: US07087626B2uspto-grants-2006_08