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

HRID 624690

반응식

HRID 624690 반응식
[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

참가 물질

5

반응물 3

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

생성물 1

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

시약·촉매·용매 1

HCID 6342Acetonitrile용매

반응 조건

온도
80 °C

실험 절차

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)

후처리

  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

출처 및 근거

ORD 기록
ord-d784bf12373e48f48cc28f5bfcc160ed
출처 데이터셋
uspto-grants-2016_04
특허 번호
US09303033B2

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