تفاعل #42651

ord-0a8c163b372448ffabb1d46cac6b07e3

المذيبات

ظروف التفاعل

درجة الحرارة
0°CELSIUS
الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىthe ice bath was removed
  2. 2
    درجة الحرارةto warm to room temperature
  3. 3
    workup.STIRRINGstir for an additional 16 hours
  4. 4
    أخرىMost of the THF was removed by rotary evaporation in vacuo
  5. 5
    أخرىthe residue was partitioned between ethyl acetate and water
  6. 6
    غسيلThe organic layer was washed successively with water, sat. NH4Cl, water, sat. NaHCO3, water and brine
  7. 7
    تجفيفThe organic layer was dried over Na2SO4
  8. 8
    ترشيحfiltered
  9. 9
    أخرىevaporated under vacuum
  10. 10
    أخرىto give an off-white solid
  11. 11
    أخرىPurification by flash chromatography through a 1.6 kg column of silica gel eluting with 4% MeOH in dichloromethane

الإجراء التجريبي

A solution of (11β,16β)-9-fluoro-16-methyl-3,20-dioxo-11,17-bis[(trimethylsilyl)oxy]pregna-1,4-dien-21-yl acetate (26 g, ˜43 mmol) in 430 mL of tetrahydrofuran (THF) was cooled to 0° C. and neat acetic acid (4.95 mL, 86.5 mmol) was added followed by dropwise addition of a 1.0 M solution of tetra-n-butylammonium fluoride in THF (43.3 mL, 43.3 mmol). After stirring at 0° C. for 4 hours, the ice bath was removed and the reaction was allowed to warm to room temperature and stir for an additional 16 hours. Most of the THF was removed by rotary evaporation in vacuo and the residue was partitioned between ethyl acetate and water. The organic layer was washed successively with water, sat. NH4Cl, water, sat. NaHCO3, water and brine. The organic layer was dried over Na2SO4, filtered and evaporated under vacuum to give an off-white solid. Purification by flash chromatography through a 1.6 kg column of silica gel eluting with 4% MeOH in dichloromethane provided 16.1 g of the title compound as a white solid.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07732432B2uspto-grants-2010_06