Pyridine → 3-Bromo-6-(3-fluorophenyl)-5-pyridin-4-ylpyrazin-2-amine

HRID 1710710ノート

反応式

HRID 1710710 の反応式
[F:1][C:2]1[CH:3]=[C:4]([C:8]2[N:13]=[C:12]([NH2:14])[CH:11]=[N:10][C:9]=2[C:15]2[CH:20]=[CH:19][N:18]=[CH:17][CH:16]=2)[CH:5]=[CH:6][CH:7]=1.N1C=CC=CC=1.[Br:27]Br>C(Cl)(Cl)Cl>[Br:27][C:11]1[C:12]([NH2:14])=[N:13][C:8]([C:4]2[CH:5]=[CH:6][CH:7]=[C:2]([F:1])[CH:3]=2)=[C:9]([C:15]2[CH:20]=[CH:19][N:18]=[CH:17][CH:16]=2)[N:10]=1

参加物

5

反応物 3

HCID 1049PyridineHCID 24408BromineHCID 160715396-(3-Fluorophenyl)-5-pyridin-4-ylpyrazin-2-amine

生成物 1

HCID 160704493-Bromo-6-(3-fluorophenyl)-5-pyridin-4-ylpyrazin-2-amine収率 24.5%

試薬・触媒・溶媒 1

HCID 6212Chloroform溶媒2 回

実験手順

To a solution of 6-(3-fluorophenyl)-5-pyridin-4-ylpyrazin-2-ylamine (Example 1, 70 mg, 0.26 mmol) in chloroform (4 mL) at 0° C. was added pyridine (22 μL, 0.27 mmol) and bromine (14 μL, 0.27 mmol). The reaction mixture was stirred at room temperature for 24 h, chloroform (20 mL) was added, the organic layer was washed with water and brine, dried (MgSO4) and evaporated. The residue was purified by silica gel flash column chromatography (dichloromethane/methanol 95:5) to provide the title compound as a red solid (22 mg, 24%).

後処理

  1. washthe organic layer was washed with water and brine
  2. dry with materialdried (MgSO4)
  3. customevaporated
  4. customThe residue was purified by silica gel flash column chromatography (dichloromethane/methanol 95:5)

出典と根拠

ORDレコード
ord-996074ccd2384285b4c49c78cd8f604e
出典データセット
uspto-grants-2010_09
特許番号
US07790728B2

反応ノート

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