반응 #88619

ord-6144d4969a1043b8b6dfe3cc948f490d

반응 조건

온도
65°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도cooled to RT
  2. 2
    세척The organic layer was washed with aq. 1N LiCl (3×30 mL)
  3. 3
    건조dried over Na2SO4
  4. 4
    농축concentrated to a residue which
  5. 5
    기타was purified by chromatography
  6. 6
    세척eluted with PE/EA (5:1 to 1:1)

실험 절차

To a solution of 1,6-dimethyl-5-nitropyrimidine-2,4(1H,3H)-dione (6 g, 0.032 mol) in DMF (20 mL) was added 2-(3-bromopropoxy)tetrahydro-2H-pyran (10.85 g, 0.049 mol) and K2CO3 (13.44 g, 0.097 mol). The reaction was heated at 65° C. for 2 h, cooled to RT then diluted with EA (20 mL) and water (20 mL). The organic layer was washed with aq. 1N LiCl (3×30 mL), dried over Na2SO4 and concentrated to a residue which was purified by chromatography eluted with PE/EA (5:1 to 1:1) to give 1,6-dimethyl-5-nitro-3-(3-((tetrahydro-2H-pyran-2-yl)oxy)propyl) pyrimidine-2,4(1H,3H)-dione (5 g, 47.1% yield) as a yellow oil. LCMS: [MH+-THP] 244 and TR=1.180 min. Used without further purification.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US09440983B2uspto-grants-2016_09