Triethylamine → 5-chloro-N-cyclopropylpyrazolo[1,5-a]pyrimidin-7-amine

HRID 624690

反応式

HRID 624690 の反応式
[Cl:1][C:2]1[CH:7]=[C:6](Cl)[N:5]2[N:9]=[CH:10][CH:11]=[C:4]2[N:3]=1.CCN(CC)CC.[CH:19]1([NH2:22])[CH2:21][CH2:20]1>C(#N)C>[Cl:1][C:2]1[CH:7]=[C:6]([NH:22][CH:19]2[CH2:21][CH2:20]2)[N:5]2[N:9]=[CH:10][CH:11]=[C:4]2[N:3]=1

参加物

5

反応物 3

HCID 8471TriethylamineHCID 69828CyclopropylamineHCID 110741545,7-Dichloropyrazolo[1,5-a]pyrimidine

生成物 1

HCID 581966065-chloro-N-cyclopropylpyrazolo[1,5-a]pyrimidin-7-amine収率 70.5%

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

反応条件

温度
80 °C

実験手順

To 5,7-dichloropyrazolo[1,5-a]pyrimidine (200 mg, 1.06 mmol) in ACN was added Et3N (148 μl, 1.06 mmol) and cyclopropylamine (75 μl, 1.06 mmol). The reaction was refluxed at 80° C. overnight. The mixture was concentrated under reduced pressure, dissolved in DCM, and washed with water. The resulting organic layer was dried over Na2SO4 and concentrated under reduced pressure to afford 156 mg of 5-chloro-N-cyclopropylpyrazolo[1,5-a]pyrimidin-7-amine (70% yield). LCMS (M+1=209)

後処理

  1. concentrationThe mixture was concentrated under reduced pressure
  2. dissolutiondissolved in DCM
  3. washwashed with water
  4. dry with materialThe resulting organic layer was dried over Na2SO4
  5. concentrationconcentrated under reduced pressure

出典と根拠

ORDレコード
ord-d784bf12373e48f48cc28f5bfcc160ed
出典データセット
uspto-grants-2016_04
特許番号
US09303033B2

関連ノート

読み込み中…