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2,5-Difluorobenzenesulfonyl chloride → N-(3-{4-[2-(ethylamino)pyrimidin-4-yl]-1-(4-methoxybenzyl)-1H-pyrazol-3-yl}phenyl)-2,5-difluorobenzenesulfonamide

HRID 45885
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HRID 45885 반응식
[NH2:1][C:2]1[CH:3]=[C:4]([C:8]2[C:12]([C:13]3[CH:18]=[CH:17][N:16]=[C:15]([NH:19][CH2:20][CH3:21])[N:14]=3)=[CH:11][N:10]([CH2:22][C:23]3[CH:28]=[CH:27][C:26]([O:29][CH3:30])=[CH:25][CH:24]=3)[N:9]=2)[CH:5]=[CH:6][CH:7]=1.[F:31][C:32]1[CH:37]=[CH:36][C:35]([F:38])=[CH:34][C:33]=1[S:39](Cl)(=[O:41])=[O:40].[Na]>N1C=CC=CC=1>[CH2:20]([NH:19][C:15]1[N:14]=[C:13]([C:12]2[C:8]([C:4]3[CH:3]=[C:2]([NH:1][S:39]([C:33]4[CH:34]=[C:35]([F:38])[CH:36]=[CH:37][C:32]=4[F:31])(=[O:41])=[O:40])[CH:7]=[CH:6][CH:5]=3)=[N:9][N:10]([CH2:22][C:23]3[CH:24]=[CH:25][C:26]([O:29][CH3:30])=[CH:27][CH:28]=3)[CH:11]=2)[CH:18]=[CH:17][N:16]=1)[CH3:21]
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

5

반응물 3

HCID 27369112,5-Difluorobenzenesulfonyl chlorideHCID 5360545SodiumHCID 671848314-[3-(3-aminophenyl)-1-(4-methoxybenzyl)-1H-pyrazol-4-yl]-N-ethylpyrimidin-2-amine

생성물 1

HCID 67185037N-(3-{4-[2-(ethylamino)pyrimidin-4-yl]-1-(4-methoxybenzyl)-1H-pyrazol-3-yl}phenyl)-2,5-difluorobenzenesulfonamide수율 91.8%

시약·촉매·용매 1

HCID 1049
Pyridine
용매

실험 절차

340 mg (0.85 mmol) of 4-[3-(3-aminophenyl)-1-(4-methoxybenzyl)-1H-pyrazol-4-yl]-N-ethylpyrimidin-2-amine were dissolved in 10 ml of dry pyridine and 114 μl (0.85 mmol) of 2,5-difluorobenzensulfonyl chloride were added. The resulting solution was stirred at room temperature overnight. The mixture was then poured into aqueous sodium hydrogenocarbonate and extracted with dichloromethane. The organic layer was finally dried over sodium sulphate and evaporated, giving 450 mg (91%) of the title compound.

후처리

  1. extractionextracted with dichloromethane
  2. dry with materialThe organic layer was finally dried over sodium sulphate
  3. customevaporated

출처 및 근거

ORD 기록
ord-4bb388d729bb4bc290abe61675222a08
출처 데이터셋
uspto-grants-2013_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08541575B2

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