반응 #93583

ord-441a4a04acb14102806f129ee8725680

용매

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    workup.ADDITIONwas added to a flask
  2. 2
    기타evacuated
  3. 3
    기타to remove oxygen
  4. 4
    workup.ADDITIONThe catalyst, 5% Pd in carbon (50% water, 19 g, Engelhard Co.), was added under an N2 atmosphere
  5. 5
    workup.ADDITIONsolid HCO2NH4 (65 g, Aldrich) was added
  6. 6
    workup.STIRRINGthe resulting mixture stirred for 1 hour
  7. 7
    온도The mixture was then slowly heated to 50° C. for 48 hours
  8. 8
    온도cooled to room temperature
  9. 9
    여과filtered through Celite (50 g)
  10. 10
    세척The solids were washed with methanol (50 mL)
  11. 11
    농축the filtrates concentrated in vacuo
  12. 12
    workup.DISSOLUTIONthe resulting solid dissolved in CH2Cl2
  13. 13
    추출The solution was extracted with saturated aqueous NH4Cl (500 mL) and saturated aqueous NaHCO3 (300 mL)
  14. 14
    기타the organic layer evaporated

실험 절차

A mixture of 1-(3,4-dimethoxyphenyl)-2-nitro-6-cyano-6-(i-propyl)-6-(3,4-dimethoxyphenyl)hexane (10, 58.7 g, 0.125 mol) and methanol (950 mL) was added to a flask, and evacuated to remove oxygen. The catalyst, 5% Pd in carbon (50% water, 19 g, Engelhard Co.), was added under an N2 atmosphere. After stirring for 10 minutes at room temperature, solid HCO2NH4 (65 g, Aldrich) was added, and the resulting mixture stirred for 1 hour. The mixture was then slowly heated to 50° C. for 48 hours, then cooled to room temperature and filtered through Celite (50 g). The solids were washed with methanol (50 mL), the filtrates concentrated in vacuo, and the resulting solid dissolved in CH2Cl2. The solution was extracted with saturated aqueous NH4Cl (500 mL) and saturated aqueous NaHCO3 (300 mL), and the organic layer evaporated to yield 1-(3,4-dimethoxyphenyl)-2-amino-6-cyano- 6-(i-propyl)-6-(3,4-dimethoxyphenyl)hexane (11, 52.3 g, MS m/e 440(M+)) as a pale yellow oil.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US04613606uspto-grants-1986_09