Pyridine → 2-[2-(1-Azabicyclo[3.3.0]octan-5-yl)ethylamino]benzonitrile

HRID 260928노트

반응식

HRID 260928 반응식
F[C:2]1[CH:9]=[CH:8][CH:7]=[CH:6][C:3]=1[C:4]#[N:5].[N:10]12[CH2:17][CH2:16][CH2:15][C:14]1([CH2:18][CH2:19][NH2:20])[CH2:13][CH2:12][CH2:11]2.N1C=CC=CC=1>O>[N:10]12[CH2:17][CH2:16][CH2:15][C:14]1([CH2:18][CH2:19][NH:20][C:2]1[CH:9]=[CH:8][CH:7]=[CH:6][C:3]=1[C:4]#[N:5])[CH2:13][CH2:12][CH2:11]2

참가 물질

5

반응물 3

HCID 1049PyridineHCID 678552-FluorobenzonitrileHCID 107969772-(Hexahydro-1H-pyrrolizin-7a-yl)ethanamine

생성물 1

HCID 107535222-[2-(1-Azabicyclo[3.3.0]octan-5-yl)ethylamino]benzonitrile수율 95.8%

시약·촉매·용매 1

HCID 962Water용매

실험 절차

2-Fluorobenzonitrile (1.00 g, 8.26 mmol) and 2-(1-azabicyclo[3.3.0]octan-5-yl)ethylamine (3.15 g, 20.4 mmol) were added into anhydrous pyridine (10.0 ml) to react the mixture in a sealed tube for 10.5 hours at 180° C. After addition of water subsequent to concentration in vacuo, the reaction mixture was extracted by ethyl acetate, dried over anhydrous sodium sulfate, concentrated in vacuo, and refined by column chromatography to afford the desired compound (2.02 g, 95.8%), as a colorless liquid.

후처리

  1. customto react the mixture in a sealed tube for 10.5 hours at 180° C
  2. concentrationto concentration in vacuo
  3. extractionthe reaction mixture was extracted by ethyl acetate
  4. dry with materialdried over anhydrous sodium sulfate
  5. concentrationconcentrated in vacuo

출처 및 근거

ORD 기록
ord-fc2793cb99ee48efbbc4e595b548bf94
출처 데이터셋
uspto-grants-1996_06
특허 번호
US05530138

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