Isopropanol → 6-Chloro-4-[(propan-2-yl)oxy]pyrido[3,2-d]pyrimidin-2-amine

HRID 1099110ノート

反応式

HRID 1099110 の反応式
[CH3:1][C:2](C)([O-:4])[CH3:3].[K+].[Cl:7][C:8]1[CH:9]=[CH:10][C:11]2[N:12]=[C:13]([NH2:23])[N:14]=[C:15](N3C=NC=N3)[C:16]=2[N:17]=1.CC(O)C>C(Cl)Cl>[Cl:7][C:8]1[CH:9]=[CH:10][C:11]2[N:12]=[C:13]([NH2:23])[N:14]=[C:15]([O:4][CH:2]([CH3:3])[CH3:1])[C:16]=2[N:17]=1

参加物

5

反応物 3

HCID 3776IsopropanolHCID 23665647Potassium tert-butoxideHCID 576983146-Chloro-4-(1H-1,2,4-triazol-1-yl)pyrido[3,2-d]pyrimidin-2-amine

生成物 1

HCID 580198016-Chloro-4-[(propan-2-yl)oxy]pyrido[3,2-d]pyrimidin-2-amine収率 67%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒2 回

実験手順

Potassium tert-butoxide (4.0 mL; 1M in THF) was added to a suspension of 6-chloro-4-[1,2,4]triazol-1-yl-pyrido[3,2-d]pyrimidin-2-ylamine (1.0 g) and 2-propanol (0.313 mL) in DCM (50 mL). After stirring at room temperature for 30 minutes, the mixture was diluted with DCM (100 mL) and washed with brine. The organic layer was dried over Na2SO4 and concentrated to afford 6-chloro-4-(2-propoxy)-pyrido[3,2-d]pyrimidin-2-ylamine as a yellow solid (0.65 g, yield: 67%) which was characterized by its mass spectrum as follows: MS (m/z) 239.1 [M+H]+.

後処理

  1. washwashed with brine
  2. dry with materialThe organic layer was dried over Na2SO4
  3. concentrationconcentrated

出典と根拠

ORDレコード
ord-a22d3f1f7cbb4ad0a3dee6584612aa7f
出典データセット
uspto-grants-2012_03
特許番号
US08143394B2

反応ノート

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