Trifluoroacetic acid → 2-amino-N-[(1R)-2-[4-benzyl-4-(N',N'-dimethylhydrazinocarbonyl)piperidin-1-yl]-1-((1H-indol-3-yl)methyl)-2-oxoethyl]-2-methylpropionamide

HRID 380665ノート

反応式

HRID 380665 の反応式
C(OC(=O)[NH:7][C:8]([C:11](=[O:45])[NH:12][CH:13]([CH2:35][C:36]1[C:44]2[C:39](=[CH:40][CH:41]=[CH:42][CH:43]=2)[NH:38][CH:37]=1)[C:14]([N:16]1[CH2:21][CH2:20][C:19]([CH2:28][C:29]2[CH:34]=[CH:33][CH:32]=[CH:31][CH:30]=2)([C:22]([NH:24][N:25]([CH3:27])[CH3:26])=[O:23])[CH2:18][CH2:17]1)=[O:15])([CH3:10])[CH3:9])(C)(C)C.FC(F)(F)C(O)=O>C(Cl)Cl>[NH2:7][C:8]([CH3:10])([CH3:9])[C:11]([NH:12][C@H:13]([CH2:35][C:36]1[C:44]2[C:39](=[CH:40][CH:41]=[CH:42][CH:43]=2)[NH:38][CH:37]=1)[C:14]([N:16]1[CH2:21][CH2:20][C:19]([CH2:28][C:29]2[CH:30]=[CH:31][CH:32]=[CH:33][CH:34]=2)([C:22]([NH:24][N:25]([CH3:27])[CH3:26])=[O:23])[CH2:18][CH2:17]1)=[O:15])=[O:45]

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 69019306(1-(2-(4-benzyl-4-(N',N'-dimethylhydrazinocarbonyl)piperidine-1-yl)-1-(1H-indol-3-ylmethyl)-2-oxoethylcarbamoyl)-1-methylethyl)carbamic acid tert-butyl ester

生成物 1

HCID 98070912-amino-N-[(1R)-2-[4-benzyl-4-(N',N'-dimethylhydrazinocarbonyl)piperidin-1-yl]-1-((1H-indol-3-yl)methyl)-2-oxoethyl]-2-methylpropionamide収率 102%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a solution of (1-(2-(4-benzyl-4-(N′,N′-dimethylhydrazinocarbonyl)piperidine-1-yl)-1-(1H-indol-3-ylmethyl)-2-oxoethylcarbamoyl)-1-methylethyl)carbamic acid tert-butyl ester (0.29 g, 0.46 mmol) in methylene chloride (3 ml) at 0° C. was added trifluoroacetic acid (3 ml) and the mixture was stirred for 30 min. The mixture was quenched with ethanol (20 ml), concentrated in vacuo and stripped three times with methylene chloride to give 0.25 g of 2-amino-N-[(1R)-2-[4-benzyl-4-(N′,N′-dimethylhydrazinocarbonyl)piperidin-1-yl]-1-((1H-indol-3-yl)methyl)-2-oxoethyl]-2-methylpropionamide as a white amorphous powder.

後処理

  1. customThe mixture was quenched with ethanol (20 ml)
  2. concentrationconcentrated in vacuo

出典と根拠

ORDレコード
ord-0656954c24a24a38ba6c4f611897b970
出典データセット
uspto-grants-2001_10
特許番号
US06303620B1

反応ノート

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