反応 #1836

ord-c9728215e0934ce58de5aa5e0e1a5863

反応方程式

C1=CCCCC1
Cyclohexene
BrBr
bromine
Cc1ccc2oc(-c3ccccc3-c3nnn[nH]3)cc2c1
2-[2-(1H-tetrazol-5-yl)phenyl]-5-methylbenzofuran
C1COCCO1
1,4-dioxane
Cc1ccc2oc(-c3ccccc3-c3nnn[nH]3)c(Br)c2c1
product
収率 85.0%
Cc1ccc2oc(-c3ccccc3-c3nnn[nH]3)c(Br)c2c1
3-Bromo-2-[2-(1H-tetrazol-5-yl)phenyl]-5-methylbenzofuran
収率 85.0%

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他A 1 L 3-neck round bottom flask equipped with a magnetic stirrer
  2. 2
    濃縮it was concentrated under vacuum to an oily residue that
  3. 3
    その他was partitioned between 100 mL of 1N aqueous sodium hydroxide and 100 mL of ether
  4. 4
    その他The aqueous layer was removed
  5. 5
    抽出extracted several times with ethyl acetate
  6. 6
    洗浄The combined extracts were washed with saturated aqueous sodium chloride
  7. 7
    乾燥dried over magnesium sulfate
  8. 8
    ろ過filtered
  9. 9
    濃縮concentrated under vacuum
  10. 10
    その他to give a white foam that
  11. 11
    その他was triturated with 100 mL of hot toluene
  12. 12
    温度The mixture was cooled in an ice bath
  13. 13
    その他the solids removed by filtration
  14. 14
    洗浄then washed with cold toluene, air
  15. 15
    その他dried
  16. 16
    その他dried under vacuum

実験手順

A 1 L 3-neck round bottom flask equipped with a magnetic stirrer, thermometer, dropping funnel and nitrogen bubbler was charged with 12.97 g (46.9 mmol) of 2-[2-(1H-tetrazol-5-yl)phenyl]-5-methylbenzofuran and 500 mL of 1,4-dioxane. To the well-stirred solution at room temperature was added a solution of 4.8 mL (93.2 mmol) of bromine in 35 mL of carbon tetrachloride dropwise over 1 hour. Cyclohexene (16 mL) was added to the reaction mixture then it was concentrated under vacuum to an oily residue that was partitioned between 100 mL of 1N aqueous sodium hydroxide and 100 mL of ether. The aqueous layer was removed, acidified with 50 mL of 2N aqueous hydrochloric acid, and extracted several times with ethyl acetate. The combined extracts were washed with saturated aqueous sodium chloride, dried over magnesium sulfate, filtered and concentrated under vacuum to give a white foam that was triturated with 100 mL of hot toluene. The mixture was cooled in an ice bath and the solids removed by filtration then washed with cold toluene, air dried and dried under vacuum to give 14.11 g (39.7 mmol, 85%) of product. 1H NMR (200 MHz,CDCl3 +1 drop DMSO-d6): 2.44 (s,3H), 7.1-7.3 (m,4H), 7.6 (m,2H), 7.86 (m,1H), 7.95 (m,1H).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US05726307uspto-grants-1998_03