تفاعل #9356

ord-5a9e347455ad418da520a0da2e094ddc

ظروف التفاعل

درجة الحرارة
0°CELSIUS
الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    استخلاصThe aqueous layer was extracted with CHCl3
  2. 2
    أخرىdried
  3. 3
    أخرىevaporated
  4. 4
    أخرىthe amide was used without further purification
  5. 5
    استخلاصextracted several times with CHCl3
  6. 6
    غسيلThe pooled fractions were washed with brine
  7. 7
    تجفيفdried over MgSO4
  8. 8
    ترشيحfiltered
  9. 9
    أخرىevaporated to dryness
  10. 10
    أخرىThe residue was purified by chromatography on SiO2

الإجراء التجريبي

5,6,7,8-Tetrahydro-naphthalen-1-ylamine (Intermediate J1, commercially available from Aldrich) (5 mL, 35.3 mmol) was dissolved in CH2Cl2 (40 mL) and treated with NEt3 (10 mL) and acetyl chloride (3.8 mL, 53 mmol) at rt for 1 h. The mixture was diluted in CHCl3 and acidified with sat NH4Cl. The aqueous layer was extracted with CHCl3. The organic fractions were combined, dried and evaporated and the amide was used without further purification. The resulting amide (35.3 mmol) in acetone (450 mL) and aqueous MgSO4 (5 g in 28 mL) at 0° C. was treated with KMnO4 (16.8 g, 105 mmol). The mixture was allowed to stir at 0° C. for 2 h. The mixture was diluted with H2O and extracted several times with CHCl3. The pooled fractions were washed with brine and dried over MgSO4, filtered and evaporated to dryness. The residue was purified by chromatography on SiO2 to give N-(8-oxo-5,6,7,8-tetrahydro-naphthalen-1-yl)-acetamide (Intermediate J2) as a yellow oil. (57%, in two 2 steps)

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07091232B2uspto-grants-2006_08