反応 #44268

ord-c0952ee84e994226b7dcb2797003c9a7

反応方程式

Brc1cnc2nnn(Cc3ccc4ncccc4c3)c2n1
6-((6-bromo-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)quinoline
Cc1c[nH]cn1
4-methyl-1H-imidazole
[Cs+].[F-]
CsF
Cc1cn(-c2cnc3nnn(Cc4ccc5ncccc5c4)c3n2)cn1
6-((6-(4-methyl-1H-imidazol-1-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)quinoline
収率 56.0%

反応条件

温度
160°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    ろ過the resulting suspension was filtered
  2. 2
    洗浄The precipitate was washed with water
  3. 3
    その他purified by column chromatography
  4. 4
    洗浄elution with methanol and dichloromethane

実験手順

A mixture of 6-((6-bromo-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)quinoline (50 mg, 0.15 mmol), 4-methyl-1H-imidazole (36 mg, 0.44 mmol) and CsF (25 mg, 0.16 mmol) in acetonitrile (1.45 mL) was heated in a microwave to 160° C. for 20 minutes. The reaction was diluted with water (5 mL) and the resulting suspension was filtered. The precipitate was washed with water and then purified by column chromatography using gradient elution with methanol and dichloromethane to afford 6-((6-(4-methyl-1H-imidazol-1-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)quinoline (28 mg, yield 56%)

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07732604B2uspto-grants-2010_06