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 480185ノート

反応式

HRID 480185 の反応式
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]

参加物

5

反応物 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

生成物 1

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

試薬・触媒・溶媒 2

HCID 6344Dichloromethane溶媒HCID 516892Sodium Bicarbonate溶媒

実験手順

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)

後処理

  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

出典と根拠

ORDレコード
ord-664a2f93ef454c8fa3de8907c22075a1
出典データセット
uspto-grants-2003_11
特許番号
US06649611B2

反応ノート

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