反応 #1265395

ord-ba49d759284942aaa41b66912a83b7d0

反応条件

温度
-70°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他the cooling bath was removed
  2. 2
    workup.ADDITIONwas poured into saturated NaHSO4
  3. 3
    抽出extracted with ethyl acetate (3×50 mL)
  4. 4
    洗浄The combined organic extracts were washed with saturated Na2CO3 (1×50 mL), brine (1×50 mL)
  5. 5
    乾燥dried over solid Na2SO4
  6. 6
    ろ過filtered
  7. 7
    濃縮The filtrate was concentrated under reduced pressure

実験手順

A solution of 4,5-dimethylthiazole (2.0 g, 17.67 mmol, 1 eq.) in dry diethyl ether (20 mL) was added slowly dropwise, over approximately 30 minutes, to a solution of butyllithium (7.8 mL, 19.44 mmol, 2.5M, 1.1 eq.) in dry diethyl ether (20 mL) at −70° C. The resultant solution was stirred at −70° C. for 30 minutes, −30° C. for 20 minutes and then re-cooled to −70° C. Dry ethyl acetate (3.11 g, 3.5 mL, 35.34 mmol, 2 eq.) was added in one portion to the deep red solution and the cooling bath was removed. After 50 minutes stirring at room temperature the reaction mixture was poured into saturated NaHSO4 and extracted with ethyl acetate (3×50 mL). The combined organic extracts were washed with saturated Na2CO3 (1×50 mL), brine (1×50 mL), dried over solid Na2SO4 and filtered. The filtrate was concentrated under reduced pressure and the resultant greenish, mobile oil was purified by column chromatography (15% ethyl acetate in hexanes) on silica gel giving a yellow oil (1.81 g, 66% yield): 1H (400 Mhz, CDCl3) δ 2.4(3H, s), 2.5(3H, s), 2.7(3H, s).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07276502B2uspto-grants-2007_10