反応 #833534

ord-d293fc55119c407e9c61fb55728968e6

反応方程式

Ic1ccccc1
Iodobenzene
c1cnc2c(c1)ccc1cccnc12
1,10-Phenanthroline
c1ccc2[nH]cnc2c1
benzimidazole
O=C([O-])[O-].[Cs+].[Cs+]
cesium carbonate
c1ccc(-n2cnc3ccccc32)cc1
1-Phenyl benzoimidazole
収率 45.0%

反応条件

温度
110°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    workup.ADDITIONIn the dark, an oven-dried 50 ml round-bottomed flask containing a stir bar
  2. 2
    その他The round-bottomed flask with the contents was sealed with septa
  3. 3
    その他degassed with argon for 15 minutes
  4. 4
    その他The reaction mixture was degassed with argon for 30 minutes
  5. 5
    温度The reaction mixture was cooled to ambient temperature
  6. 6
    濃縮concentrated in vacuo
  7. 7
    workup.ADDITION10 ml of ethyl acetate was added into the concentrated reaction mixture
  8. 8
    ろ過It was then filtered
  9. 9
    洗浄washed with 30 ml of ethyl acetate
  10. 10
    濃縮The filtrate was concentrated under vacuo
  11. 11
    その他to give the crude product
  12. 12
    その他The crude product was purified by column chromatography on silica gel (40% ethyl acetate

実験手順

In the dark, an oven-dried 50 ml round-bottomed flask containing a stir bar was charged with CuI (0.171 g, 0.1 eq.), benzimidazole (1.273 g, 1.2 eq.), and cesium carbonate (6.138 g, 2.1 eq.) respectively. The round-bottomed flask with the contents was sealed with septa and degassed with argon for 15 minutes. Iodobenzene (1 ml, 1 eq.), 1,10-Phenanthroline (0.323 g, 0.2 eq.), and dimethylformamide (25 ml) were then successively added into the round-bottomed flask under a continuous flow of argon. The reaction mixture was degassed with argon for 30 minutes. The reaction was stirred with heating via an oil bath at 110° C. for 24 hours in the dark under nitrogen. The reaction mixture was cooled to ambient temperature and concentrated in vacuo. 10 ml of ethyl acetate was added into the concentrated reaction mixture. It was then filtered and washed with 30 ml of ethyl acetate. The filtrate was concentrated under vacuo to give the crude product. The crude product was purified by column chromatography on silica gel (40% ethyl acetate:60% hexane as the eluent) providing 0.780 g of 1-Phenyl benzoimidazole (45% yield) as yellow liquid.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07393599B2uspto-grants-2008_07