反応 #2651

ord-443e36063c0a47edae71957a9c2af350

反応方程式

O[C@@H]1C=C[C@H](OCc2ccccc2)C1
Cis-4-benzyloxy-cyclopent-2-enol
CCN(CC)CC
triethylamine
C=COC(C)=O
vinyl acetate
ClC(Cl)Cl
chloroform
ClC(Cl)Cl
chloroform
O[C@@H]1C=C[C@H](OCc2ccccc2)C1
(-)-cis-4-benzyloxy-cyclopent-2-enol
収率 29.0%
CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1
(-)-acetic acid cis-4-benzyloxy-cyclopent-2-enyl ester
収率 70.0%

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    ろ過The reaction is then filtered through diatomaceous earth
  2. 2
    濃縮the filtrate is concentrated under vacuum
  3. 3
    その他The products are separated by chromatography on silica gel (20% ethyl acetate/hexane)

実験手順

Cis-4-benzyloxy-cyclopent-2-enol (500 mg, prepared in example 16) is dissolved in tert-butyl methyl ether (8.6 mL, anhydrous). To the solution is added triethylamine (0.7 eq), pancreatin (3 wt eq, available from Sigma Chemical Company), and vinyl acetate (5 eq). The reaction is allowed to stir for 7 hours at room temperature. The reaction is then filtered through diatomaceous earth and the filtrate is concentrated under vacuum. The products are separated by chromatography on silica gel (20% ethyl acetate/hexane) to provide (-)-cis-4-benzyloxy-cyclopent-2-enol (A) (147 mg, 29% yield) [α]20D -12°, (c=1.09, chloroform), and (-)-acetic acid cis-4-benzyloxy-cyclopent-2-enyl ester (B) (427 mg, 70% yield),[α]20D =-5.2°, (c=0.97, chloroform), 1 H NMR (CDCl3) δ 7.3 (m, 5H), 6.13 (d, 1H, J=5 Hz), 5.99 (d, 1H, J=5 Hz), 5.5 (m, 1H), 4.59 (d, 1H, J=11.8 Hz), 4.54 (d, 1H, J=11.8 Hz), 4.5 (m, 1H), 2.78 (d appt, 1H, J=7.2, 14.3 Hz), 2.05 (s, 3H), 1.76 (d appt, 1H, J=4.4, 14.3 Hz); 13C NMR (CDCl3) δ171.1, 138.5, 136.4, 133.1, 128.7, 128, 127.9, 81.4, 77.1, 71.2, 37.8, 21.4.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US05728899uspto-grants-1998_03