반응 #1153156

ord-a1291f80efb845d6bd83883244473bf6

반응 방정식

N[C@H]1CCCN[C@H]1c1ccccc1
(2S,3S)-(−)-3-amino-2-phenylpiperidine
O=C(Cl)OCc1ccccc1
benzyl chloroformate
CCN(C(C)C)C(C)C
diisopropylethylamine
O=C(N[C@H]1CCCN[C@H]1c1ccccc1)OCc1ccccc1
title compound
수율 80.2%
O=C(N[C@H]1CCCN[C@H]1c1ccccc1)OCc1ccccc1
(2S,3S)-3-Benzyloxycarbonylamino-2-phenylpiperidine
수율 80.2%

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타quenched by addition of water
  2. 2
    기타The mixture was separated
  3. 3
    세척The organic layers were successively washed with a portion of brine
  4. 4
    건조dried over sodium sulfate
  5. 5
    기타evaporated
  6. 6
    기타The residue was purified by flash chromatography (5% methanol in methylene chloride)

실험 절차

To a solution of (2S,3S)-(−)-3-amino-2-phenylpiperidine (152 mg, 0.86 mmole) (L-tartaric acid salt, [a]D=−57.1 (EtOH, c=0.1138)) in methylene chloride (10 mL) at room temperature was added benzyl chloroformate (0.123 mL, 0.86 mmole) and diisopropylethylamine (0.45 mL, 2.58 mmole). The reaction was stirred for 16 hours and was then diluted with methylene chloride and quenched by addition of water. The mixture was separated and the aqueous was reextracted with 2 additional aliquots of methylene chloride. The organic layers were successively washed with a portion of brine, dried over sodium sulfate, combined and evaporated. The residue was purified by flash chromatography (5% methanol in methylene chloride) to afford 214 mg (80%) of the title compound. NMR (CDCl3): δ 1.55 (br, d, J=9 Hz, 1 H), 1.6-1.9 (m, 2 H), 2.02 (br. d, J=9 Hz, 1 H), 2.79 (dd, J=9 and 10 Hz, 1 H), 3.22 (dd, J=1 and 10 Hz, 1 H), 3.91 (br. s, 1 H), 4.01 (dd, J=1 and 8 Hz, 1 H), 4.89 (s, 2 H), 5.65 and 5.88 (2 br. s, 1 H), 7.1-7.4 (m, 10 H).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US06241964B1uspto-grants-2001_06