تفاعل #2646

ord-23a5242235f843fa9d331c47debf3305

معادلة التفاعل

ClC(Cl)Cl
chloroform
O[C@@H]1C=C[C@H](OC2CCCCO2)C1
(-)-cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enol
ClC(Cl)Cl
chloroform
CCN(CC)CC
triethylamine
C=COC(C)=O
vinyl acetate
O[C@@H]1C=C[C@H](OC2CCCCO2)C1
Cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enol
CC(=O)O[C@@H]1C=C[C@H](OC2CCCCO2)C1
(-)-acetic acid cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enyl ester
المردود 45.0%

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 (10% to 20% ethyl acetate/hexane)

الإجراء التجريبي

Cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enol (1.091 g, 5.92 mmol, prepared in example 6) is dissolved in tert-butyl methyl ether (8.6 mL, anhydrous). To the solution is added triethylamine (0.59 mL, 4.2 mmol), pancreatin (3.2 g, available from Sigma Chemical Company), and vinyl acetate (2.7 mL, 29 mmol). 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 (10% to 20% ethyl acetate/hexane) to provide (-)-acetic acid cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enyl ester (B, 601 mg, 45% yield, 91% ee) [α]D =-19.8°,(c=1.00, chloroform) as a yellow oil and (-)-cis-4-(tetrahydro-pyran-2-yloxy)-cyclopent-2-enol (A, 560 mg, 50% yield, 94% ee), [α]D =-9.9°, (c=1.06, chloroform) as a yellow oil.

المصدر

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