تفاعل #75748

ord-06e00cba0af442d88b19a2cc5c5dcb62

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    ترشيحThe reaction mixture was filtered
  2. 2
    أخرىto remove the catalyst
  3. 3
    تركيزthe filtrate was concentrated under vacuum
  4. 4
    workup.ADDITIONa small amount of 10% sodium hydroxide was added
  5. 5
    استخلاصThe resulting precipitate was extracted with dichloromethane
  6. 6
    استخلاصThe dichloromethane extract
  7. 7
    تجفيفwas dried over magnesium sulfate
  8. 8
    تركيزthen concentrated under vacuum
  9. 9
    أخرىThe residue was purified by flash chromatography (silica gel eluting with 5% methanol in dichloromethane containing 0.5% ammonium hydroxide)
  10. 10
    تركيزThe eluant was concentrated under vacuum
  11. 11
    أخرىThe residue was recrystallized from ethyl acetate

الإجراء التجريبي

A catalytic amount of platinum oxide was added to a solution of 1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine (0.46 g) in trifluoroacetic acid (10 mL). The reaction mixture was reduced on a Parr apparatus under 45 psi (3.15 Kg/cm2) hydrogen pressure for 4 hours. The reaction mixture was filtered to remove the catalyst and the filtrate was concentrated under vacuum. The residue was combined with aqueous sodium bicarbonate then a small amount of 10% sodium hydroxide was added. The resulting precipitate was extracted with dichloromethane. The dichloromethane extract was dried over magnesium sulfate then concentrated under vacuum. The residue was purified by flash chromatography (silica gel eluting with 5% methanol in dichloromethane containing 0.5% ammonium hydroxide). The eluant was concentrated under vacuum. The residue was recrystallized from ethyl acetate to provide 6,7,8,9-tetrahydro-1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine as a solid, m.p. 222-226° C. Analysis: Calculated for C13H19N5: %C, 63.65; %H, 7.81; %N, 28.55. Found: %C, 63.07; %H, 7.51; %N, 28.00.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US06699878B2uspto-grants-2004_03