Pyrazole → 1-{4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl}-1H-pyrazole

HRID 483874

반응식

HRID 483874 반응식
[Br-].[N:2]1[CH:7]=[CH:6][CH:5]=[N:4][C:3]=1[N:8]1[CH2:17][CH2:16][N+:11]2([CH2:15][CH2:14][CH2:13][CH2:12]2)[CH2:10][CH2:9]1.[NH:18]1[CH:22]=[CH:21][CH:20]=[N:19]1.C(=O)([O-])[O-].[K+].[K+]>CN(C)C=O>[N:4]1[CH:5]=[CH:6][CH:7]=[N:2][C:3]=1[N:8]1[CH2:9][CH2:10][N:11]([CH2:15][CH2:14][CH2:13][CH2:12][N:18]2[CH:22]=[CH:21][CH:20]=[N:19]2)[CH2:16][CH2:17]1

참가 물질

5

반응물 3

HCID 1048PyrazoleHCID 11430Potassium CarbonateHCID 6575058-Aza-5-azoniaspiro(4.5)decane, 8-(2-pyrimidinyl)-, bromide (1:1)

생성물 1

HCID 110443661-{4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl}-1H-pyrazole

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

반응 조건

온도
140 °C

실험 절차

A mixture of 730 g (3.59 moles) of 8-(2-pyrimidinyl)-8-aza-5-azoniaspiro[4,5]decane bromide, 275 g (4.05 moles) of pyrazole and 745 g (5.4 moles) of potassium carbonate in 3 1 of dimethylformamide is heated to 140° C. for 14 hours. The mixture is evaporated under vacuum, chloroform is added, the solution is washed with water, dried over sodium sulfate and evaporated under vacuum, and 650 g (94%) of 1-{4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl}-1H-pyrazole are obtained in liquid form.

후처리

  1. customThe mixture is evaporated under vacuum, chloroform
  2. additionis added
  3. washthe solution is washed with water
  4. dry with materialdried over sodium sulfate
  5. customevaporated under vacuum, and 650 g (94%) of 1-{4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl}-1H-pyrazole
  6. customare obtained in liquid form

출처 및 근거

ORD 기록
ord-00438c32cf89405f95ce1ee33dcba21e
출처 데이터셋
uspto-grants-1993_07
특허 번호
US05227486

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