Water → 5-Bromo-6-chloro-2-(1H-pyrazol-1-yl)-4-pyrimidinamine

HRID 2401163

反応式

HRID 2401163 の反応式
[Br:1][C:2]1[C:3]([NH2:12])=[N:4][C:5](S(C)=O)=[N:6][C:7]=1[Cl:8].[NH:13]1[CH:17]=[CH:16][CH:15]=[N:14]1.C(=O)([O-])[O-].[Cs+].[Cs+].O>CN(C=O)C>[Br:1][C:2]1[C:3]([NH2:12])=[N:4][C:5]([N:13]2[CH:17]=[CH:16][CH:15]=[N:14]2)=[N:6][C:7]=1[Cl:8]

参加物

6

反応物 4

HCID 962WaterHCID 1048PyrazoleHCID 10796Cesium carbonateHCID 866770165-Bromo-6-chloro-2-methanesulfinylpyrimidin-4-amine2 回

生成物 1

HCID 866770175-Bromo-6-chloro-2-(1H-pyrazol-1-yl)-4-pyrimidinamine収率 65%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

1 g (3.7 mmol) of 5-bromo-6-chloro-2-(methylsulfinyl)pyrimidine-4-amine (intermediate 2) was suspended in 10 ml of DMF. To this suspension were added 0.33 g (4.8 mmol) de pyrazole and 0.8 g of cesium carbonate. The reaction mixture was turned immediately light yellow color and allowed to stir at room temperature for about 1 to 2 hours. After nearly complete conversion to the corresponding monosubstituted derivative as was indicated by TLC the solution was poured onto 100 ml of cool water. The formed precipitated was filtered, washed with water and dried to afford 0.66 g (65%) of the desired product.

後処理

  1. customThe formed precipitated
  2. filtrationwas filtered
  3. washwashed with water
  4. customdried

出典と根拠

ORDレコード
ord-be51a176488d42638229ef21fd1ee146
出典データセット
uspto-grants-2014_08
特許番号
US08796284B2

関連ノート

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