반응 #80593

ord-d739180875594717a1f57f80fb74b667

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    workup.ADDITIONwas added over 15 minutes
  2. 2
    온도the reaction mixture was heated to 90°-95° C
  3. 3
    workup.WAITAfter 20 hours
  4. 4
    온도the reaction mixture was cooled to room temperature
  5. 5
    여과After filtration
  6. 6
    세척the residue was washed with a mixture of methylene chloride/methanol (2/1).The combined filtrates
  7. 7
    농축were concentrated in vacuo
  8. 8
    workup.STIRRINGthe resulting yellowish solid was stirred with a mixture of hexane/ether (2/1, 1000 mL)
  9. 9
    여과The product was filtered
  10. 10
    세척washed with more of hexane/ether (2/1)
  11. 11
    기타The pale yellow solid 3,4-methylenedioxy-N-[4-(methylsulfonyl)phenyl]benzenecarboximidamide (4.8g, 91%) was used in the next reaction without further purification

실험 절차

To a suspension of (4-methylsulfonyl)aniline (2.82 g, 16.5 mmol) in toluene (150 mL), trimethylaluminum (2M solution in toluene, 12.5 mL, 24.7 mmol) was added over 15 minutes. The reaction mixture was warmed to room temperature and stirred for 2.5 hours. A solution of piperonylonitrile (4.85 g, 33 mmol) in toluene (100 mL) was added over 10 minutes and the reaction mixture was heated to 90°-95° C. After 20 hours, the reaction mixture was cooled to room temperature and poured over a slurry of silica gel in chloroform. After filtration, the residue was washed with a mixture of methylene chloride/methanol (2/1).The combined filtrates were concentrated in vacuo and the resulting yellowish solid was stirred with a mixture of hexane/ether (2/1, 1000 mL). The product was filtered and washed with more of hexane/ether (2/1). The pale yellow solid 3,4-methylenedioxy-N-[4-(methylsulfonyl)phenyl]benzenecarboximidamide (4.8g, 91%) was used in the next reaction without further purification: mp (DSC) 214° C. Anal. Calc'd. for C15H14N2SO4 : C, 56.59, H, 4.43, N, 8.80. Found: C, 56.33, H, 4.28, N, 8.66.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US05616601uspto-grants-1997_04