Trifluoroacetic acid → (2R)-3-Amino-N-(5-chloro-2-{2-[4-(4-fluoro-benzyl)-2-methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-propionamide

HRID 480185노트

반응식

HRID 480185 반응식
C(OC(=O)[NH:7][CH2:8][CH2:9][C:10](=[O:38])[NH:11][C:12]1[CH:17]=[C:16]([Cl:18])[CH:15]=[CH:14][C:13]=1[O:19][CH2:20][C:21]([N:23]1[CH2:28][CH2:27][N:26]([CH2:29][C:30]2[CH:35]=[CH:34][C:33]([F:36])=[CH:32][CH:31]=2)[CH2:25][CH:24]1[CH3:37])=[O:22])(C)(C)C.FC(F)(F)C(O)=O>C(Cl)Cl.C(=O)([O-])O.[Na+]>[NH2:7][CH2:8][CH2:9][C:10]([NH:11][C:12]1[CH:17]=[C:16]([Cl:18])[CH:15]=[CH:14][C:13]=1[O:19][CH2:20][C:21]([N:23]1[CH2:28][CH2:27][N:26]([CH2:29][C:30]2[CH:31]=[CH:32][C:33]([F:36])=[CH:34][CH:35]=2)[CH2:25][C@H:24]1[CH3:37])=[O:22])=[O:38]

참가 물질

5

반응물 2

HCID 6422Trifluoroacetic acidHCID 69911989[2-(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-2-methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenylcarbamoyl)-ethyl]-carbamic acid tert-butyl ester

생성물 1

HCID 12112108(2R)-3-Amino-N-(5-chloro-2-{2-[4-(4-fluoro-benzyl)-2-methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-propionamide수율 74.5%

시약·촉매·용매 2

HCID 6344Dichloromethane용매HCID 516892Sodium Bicarbonate용매

실험 절차

To a solution of [2-(5-chloro-2-{2-[4-(4-fluoro-benzyl)-2-methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenylcarbamoyl)-ethyl]-carbamic acid tert-butyl ester (0.110 g, 0.2 mmol) in methylene chloride (3 mL) was added trifluoroacetic acid (0.50 mL). The reaction was stirred for 2 hours at ambient temperature then diluted with saturated aqueous sodium hydrogen carbonate. The mixture was extracted with methylene chloride and the combined organics were dried over magnesium sulfate, filtered and concentrated in vacuo to give the title compound (0.069 g)

후처리

  1. extractionThe mixture was extracted with methylene chloride
  2. dry with materialthe combined organics were dried over magnesium sulfate
  3. filtrationfiltered
  4. concentrationconcentrated in vacuo

출처 및 근거

ORD 기록
ord-664a2f93ef454c8fa3de8907c22075a1
출처 데이터셋
uspto-grants-2003_11
특허 번호
US06649611B2

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