تفاعل #2651

ord-443e36063c0a47edae71957a9c2af350

معادلة التفاعل

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
المردود 29.0%
CC(=O)O[C@@H]1C=C[C@H](OCc2ccccc2)C1
(-)-acetic acid cis-4-benzyloxy-cyclopent-2-enyl ester
المردود 70.0%

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    ترشيحThe reaction is then filtered through diatomaceous earth
  2. 2
    تركيزthe filtrate is concentrated under vacuum
  3. 3
    أخرىThe products are separated by chromatography on silica gel (20% ethyl acetate/hexane)

الإجراء التجريبي

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.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US05728899uspto-grants-1998_03