4-((S)-4-tert-Butoxycarbonyl-2-{[5-(3,3-dimethyl-2-oxo-butoxy)-1-phenyl-1H-pyrazole-3-carbonyl]-amino}-butyryl)-piperazine-1-carboxylic acid benzyl ester → (S)-4-{[5-(3,3-Dimethyl-2-oxo-butoxy)-1-phenyl-1H-pyrazole-3-carbonyl]-amino}-5-oxo-5-piperazin-1-yl-pentanoic acid tert-butyl ester

HRID 1908649노트

반응식

HRID 1908649 반응식
C(OC([N:11]1[CH2:16][CH2:15][N:14]([C:17](=[O:50])[C@@H:18]([NH:28][C:29]([C:31]2[CH:35]=[C:34]([O:36][CH2:37][C:38](=[O:43])[C:39]([CH3:42])([CH3:41])[CH3:40])[N:33]([C:44]3[CH:49]=[CH:48][CH:47]=[CH:46][CH:45]=3)[N:32]=2)=[O:30])[CH2:19][CH2:20][C:21]([O:23][C:24]([CH3:27])([CH3:26])[CH3:25])=[O:22])[CH2:13][CH2:12]1)=O)C1C=CC=CC=1>C(O)C.[Pd]>[C:24]([O:23][C:21](=[O:22])[CH2:20][CH2:19][C@H:18]([NH:28][C:29]([C:31]1[CH:35]=[C:34]([O:36][CH2:37][C:38](=[O:43])[C:39]([CH3:40])([CH3:41])[CH3:42])[N:33]([C:44]2[CH:49]=[CH:48][CH:47]=[CH:46][CH:45]=2)[N:32]=1)=[O:30])[C:17](=[O:50])[N:14]1[CH2:15][CH2:16][NH:11][CH2:12][CH2:13]1)([CH3:25])([CH3:26])[CH3:27]

참가 물질

4

반응물 1

HCID 669201124-((S)-4-tert-Butoxycarbonyl-2-{[5-(3,3-dimethyl-2-oxo-butoxy)-1-phenyl-1H-pyrazole-3-carbonyl]-amino}-butyryl)-piperazine-1-carboxylic acid benzyl ester

생성물 1

HCID 66920033(S)-4-{[5-(3,3-Dimethyl-2-oxo-butoxy)-1-phenyl-1H-pyrazole-3-carbonyl]-amino}-5-oxo-5-piperazin-1-yl-pentanoic acid tert-butyl ester수율 115.7%

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 702Ethanol용매

실험 절차

To a solution of 4.4 g 4-((S)-4-tert-Butoxycarbonyl-2-{[5-(3,3-dimethyl-2-oxo-butoxy)-1-phenyl-1H-pyrazole-3-carbonyl]-amino}-butyryl)-piperazine-1-carboxylic acid benzyl ester in 40 ml ethanol were added 0.9 g Pd/C (10%) and the suspension stirred under an atmosphere of hydrogen (3 bar) for 24 h. It was filtrated, washed with ethanol and the solvent evaporated to give the title compound as colorless oil (4.1 g).

후처리

  1. filtrationIt was filtrated
  2. washwashed with ethanol
  3. customthe solvent evaporated

출처 및 근거

ORD 기록
ord-5cafd9a65cf94b8081a84c43cd1b8d49
출처 데이터셋
uspto-grants-2013_12
특허 번호
US08598179B2

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