반응 #83118

ord-8d7c65912f004e68ba52bca32d85ce44

반응 조건

온도
0°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    workup.STIRRINGThis solution was stirred for one hour at 0° C.
  2. 2
    기타at room temperature for four hours before leaving it at 4° C. overnight
  3. 3
    여과The mixture was filtered
  4. 4
    세척the precipitate washed with cold ethyl acetate (30 mL)
  5. 5
    workup.WAITThe mixture was left
  6. 6
    workup.STIRRINGto stir for 48 hours at room temperature
  7. 7
    여과The reaction mixture was filtered
  8. 8
    세척the residue washed with cold ethyl acetate (2×30 mL)

실험 절차

To a solution of N-[(9H-fluoren-9-ylmethyloxy)carbonyl]-α-methyl-DL-tryptophan (8.80 g, 20 mmol) in dry ethyl acetate (350 mL) was added pentafluorophenol (3.68 g, 20 mmol) and stirred for 10 minutes. The reaction mixture was cooled to 0° C. and a solution of dicyclohexylcarbodiimide (20 mmol) in ethyl acetate (25 mL) was added dropwise. This solution was stirred for one hour at 0° C. then at room temperature for four hours before leaving it at 4° C. overnight. The mixture was filtered and the precipitate washed with cold ethyl acetate (30 mL) and a solution of 2-phenethylamine (2.66 g, 22 mmol) in ethyl acetate (30 mL) was added dropwise to the combined filtrates. The mixture was left to stir for 48 hours at room temperature. The reaction mixture was filtered and the residue washed with cold ethyl acetate (2×30 mL) to give the title compound (3.73 g, 75%). The filtrates were combined and the solvent removed in vacuo and taken up again in ethyl acetate (5 mL) to give a second crop of 1.67 g (15%), a total of 90% yield as a white solid, mp 179°-181° C. (EtOAc); IR (film) 1708, 1652 cm-1 ; NMR (DMSO d6) δ1.30 (3H, s), 2.64 (2H, t, J 7.2Hz), 3.2-3.3 (4H, m), 4.19 (1H, t, J 6.7Hz), 4.25-4.40 (2H, m), 6.9-7.9 (20 H, m), 10.8 (1H, s).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US05622983uspto-grants-1997_04