反応 #10286

ord-17af3ceeed304966aae96f3eace54d08

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    温度the mixture was heated
  2. 2
    温度to reflux
  3. 3
    その他the reaction
  4. 4
    workup.STIRRINGThe reaction mixture was stirred at room temperature for 16 hrs
  5. 5
    その他crushed ice
  6. 6
    抽出The mixture was extracted with two 50 mL portions ethyl acetate
  7. 7
    洗浄The organic phase was washed with 25 mL saturated sodium chloride
  8. 8
    乾燥dried (magnesium sulfate)
  9. 9
    濃縮concentrated under reduced pressure

実験手順

To a suspension of 0.85 g (34.6 mmole) magnesium turnings in 25 mL tetrahydrofuran was added 5 mL of a solution of 5 g (28.8 mmole) 1-bromo-4-tert-butylbenzene in 25 mL tetrahydrofuran. One iodine crystal and 1,2-dibromoethane (0.3 mL) was added and the mixture was heated to reflux to initiate the reaction. The rest of the 1-bromo-4-tert-butylbenzene solution was then added dropwise and the reaction mixture was stirred at room temperature for 1 hr. The remaining magnesium was allowed to settle and the supernatant was added in portions to a cooled, previously prepared mixture of 8 g (27.4 mmole) ((S)-1-methyl-2-morpholin-4-yl-2-oxoethyl)-carbamic acid benzyl ester n in 30 mL tetrahydrofuran and 30 mL (60 mmole) 2M isopropylmagnesium chloride in diethyl ether. The reaction mixture was stirred at room temperature for 16 hrs. The mixture was then added to a well-stirred mixture of 100 mL 5% hydrochloric acid and crushed ice. The mixture was extracted with two 50 mL portions ethyl acetate. The organic phase was washed with 25 mL saturated sodium chloride, dried (magnesium sulfate) and concentrated under reduced pressure. (S)-2-(4-tert-Butylphenyl)-1-methyl-2-oxoethyl]-carbamic acid benzyl ester o was isolated as a solid, 9.2 g. m.p. 156–158° C.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07094778B2uspto-grants-2006_08