반응 #1532719

ord-7a16e7b31bad44ecb2154a18c0c8c7c6

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타The reaction mixture thinned to form a pale green, nearly clear solution
  2. 2
    기타to form a pale yellow suspension
  3. 3
    온도the reaction mixture was heated
  4. 4
    온도at gentle reflux for 3.5 hours
  5. 5
    온도After cooling
  6. 6
    기타a precipitate of white solid was removed by filtration
  7. 7
    추출Concentration of the acetonitrile mother liquor and then dilution with water (400 mL) was followed by extraction three times with ethyl ether (700 mL total)
  8. 8
    농축The ethyl ether phase was concentrated to a reduced volume (75 mL) from which
  9. 9
    기타precipitated an-off white solid (3.75 g), which
  10. 10
    여과was collected by filtration
  11. 11
    농축The ether mother liquor was further concentrated

실험 절차

To a suspension of ethyl 1-(3-chloro-2-pyridinyl)-3-pyrazolidinone-5-carboxylate (i.e. the product of Step A) (27 g, 100 mmol) stirred in dry acetonitrile (200 mL) was added sulfuric acid (20 g, 200 mmol) in one portion. The reaction mixture thinned to form a pale green, nearly clear solution before thickening again to form a pale yellow suspension. Potassium persulfate (33 g, 120 mmol) was added in one portion, and then the reaction mixture was heated at gentle reflux for 3.5 hours. After cooling using an ice bath, a precipitate of white solid was removed by filtration and discarded. Concentration of the acetonitrile mother liquor and then dilution with water (400 mL) was followed by extraction three times with ethyl ether (700 mL total). The ethyl ether phase was concentrated to a reduced volume (75 mL) from which precipitated an-off white solid (3.75 g), which was collected by filtration. The ether mother liquor was further concentrated to yield a second crop of an off-white precipitate (4.2 g), which was collected by filtration. Further precipitation of an off-white solid (4.5 g) from the aqueous phase yielded a combined total of 12.45 g of the title compound.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07666882B2uspto-grants-2010_02