Triethylamine → 2-chloro-N-cyclopropyl-5-fluoropyrimidin-4-amine

HRID 2400334노트

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HRID 2400334 반응식
[Cl:1][C:2]1C=[C:6](Cl)[C:5]([F:9])=[CH:4][N:3]=1.CC[N:12](CC)CC.[CH:17]1([NH2:20])[CH2:19][CH2:18]1>CC#N>[Cl:1][C:2]1[N:12]=[C:6]([NH:20][CH:17]2[CH2:19][CH2:18]2)[C:5]([F:9])=[CH:4][N:3]=1

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 69828CyclopropylamineHCID 220610192,4-Dichloro-5-fluoropyridine

생성물 1

HCID 53067942-chloro-N-cyclopropyl-5-fluoropyrimidin-4-amine수율 81.7%

시약·촉매·용매 1

HCID 6342Acetonitrile용매2회

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온도
0 °C

실험 절차

To 2,4 dichloro-5-fluoropyridine (1 g, 6 mmol) dissolved in CH3CN (8 ml) cooled in an ice bath was added Et3N (1.16 ml, 8.4 mmol) and cyclopropylamine (0.29 ml, 8.4 mmol) in CH3CN (2 ml). Reaction stirred 0° C. for 2 hours, evaporated water added and reaction extracted with EtOAc (×3). The organic fractions were combined washed with brine, dried over MgSO4, filtered and concentrated under reduced pressure to give the product (0.92 g).

후처리

  1. temperaturecooled in an ice bath
  2. customReaction
  3. customevaporated water
  4. additionadded
  5. customreaction
  6. extractionextracted with EtOAc (×3)
  7. washThe organic fractions were combined washed with brine
  8. dry with materialdried over MgSO4
  9. filtrationfiltered
  10. concentrationconcentrated under reduced pressure

출처 및 근거

ORD 기록
ord-5e0cb507574b4ece835653e28df8ff43
출처 데이터셋
uspto-grants-2014_08
특허 번호
US08796244B2

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