반응 #352180

ord-bbae8b7c8b2e4a4c887fd126b97d206f

반응 방정식

C=CCN(CCC)C1COc2cccc(OS(=O)(=O)C(F)(F)F)c2C1
3-(N-Allyl-N-n-propylamino)-5-trifluoromethanesulfonyloxychroman
[Cl-].[Li+]
LiCl
CN(C)C=O
DMF
[CH3][Sn]([CH3])([CH3])[CH3]
Tetramethyltin
C=CCN(CCC)C1COc2cccc(C(C)=O)c2C1
5-acetyl-3-(N-allyl-N-n-propylamino)-chroman
수율 39.0%

반응 조건

온도
120°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타The flask was evacuated
  2. 2
    기타followed by inlet of CO (three times)
  3. 3
    기타The solvent was evaporated
  4. 4
    기타the residue was partitioned between aqueous NH3 (2M) and CH2Cl2 (3×15 mL)
  5. 5
    건조the organic phases were dried (Na2SO4)
  6. 6
    여과filtered
  7. 7
    농축concentrated in vacuo

실험 절차

3-(N-Allyl-N-n-propylamino)-5-trifluoromethanesulfonyloxychroman (0.28 g, 0.74 mmol), LiCl (0.097 g, 2.3 mmol), PdCl2 (dppf) (0.031 g, 0.04 mmol) and 2.6-di-t-butyl-4-methylphenol (0.005 g) were dissolved in DMF (5.0 mL) in a three-necked round-bottom flask (50 mL) with a magnetic stirrer. The flask was evacuated, followed by inlet of CO (three times). Tetramethyltin (0.12 mL, 0.89 mmol) was added and then the mixture was stirred under an atmosphere of CO (1 atm) at 120° C. (oilbath temp) for 4 hours. The solvent was evaporated, the residue was partitioned between aqueous NH3 (2M) and CH2Cl2 (3×15 mL) and the organic phases were dried (Na2SO4), filtered and concentrated in vacuo. Column chromatography on silica with THF-n-hexane (1:9) as eluent afforded 5-acetyl-3-(N-allyl-N-n-propylamino)-chroman (0.078 g, 39% yield) as an oil. The base was precipitated from an ether solution by adding a slight excess of HCl (approx. 3M in ether). The crude salt was collected and dried in vacuo at 40° C. to give a white amorphous powder. Mp 125°-127° C. PdCl2 (dppf)=dichloro[1,1'-bis(diphenylphosphino)-ferrocene]-palladium (II).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US05646309uspto-grants-1997_07