Pyridine → 3'-{({2-[4-(Aminosulfonyl)phenyl]ethyl}[(benzyloxy)acetyl]amino)methyl}-N-[2-(1-pyrrolidinyl)ethyl][1,1'-biphenyl]-3-carboxamide

HRID 9777

反応式

HRID 9777 の反応式
N1C=CC=CC=1.[CH2:7]([O:14][CH2:15][C:16](Cl)=[O:17])[C:8]1[CH:13]=[CH:12][CH:11]=[CH:10][CH:9]=1.[NH2:19][S:20]([C:23]1[CH:28]=[CH:27][C:26]([CH2:29][CH2:30][NH:31][CH2:32][C:33]2[CH:34]=[C:35]([C:39]3[CH:44]=[CH:43][CH:42]=[C:41]([C:45]([NH:47][CH2:48][CH2:49][N:50]4[CH2:54][CH2:53][CH2:52][CH2:51]4)=[O:46])[CH:40]=3)[CH:36]=[CH:37][CH:38]=2)=[CH:25][CH:24]=1)(=[O:22])=[O:21]>CN(C=O)C.O>[NH2:19][S:20]([C:23]1[CH:24]=[CH:25][C:26]([CH2:29][CH2:30][N:31]([CH2:32][C:33]2[CH:34]=[C:35]([C:39]3[CH:44]=[CH:43][CH:42]=[C:41]([C:45]([NH:47][CH2:48][CH2:49][N:50]4[CH2:54][CH2:53][CH2:52][CH2:51]4)=[O:46])[CH:40]=3)[CH:36]=[CH:37][CH:38]=2)[C:16](=[O:17])[CH2:15][O:14][CH2:7][C:8]2[CH:13]=[CH:12][CH:11]=[CH:10][CH:9]=2)=[CH:27][CH:28]=1)(=[O:22])=[O:21]

参加物

6

反応物 3

HCID 1049PyridineHCID 177085Benzyloxyacetyl chlorideHCID 102392483'-[{2-[4-(aminosulfonyl)phenyl]ethyl}aminomethyl]-N-[2-(1-pyrrolidinyl)ethyl][1,1'-biphenyl]-3-carboxamide

生成物 1

HCID 102831223'-{({2-[4-(Aminosulfonyl)phenyl]ethyl}[(benzyloxy)acetyl]amino)methyl}-N-[2-(1-pyrrolidinyl)ethyl][1,1'-biphenyl]-3-carboxamide

試薬・触媒・溶媒 2

HCID 962Water溶媒HCID 6228Dimethylformamide溶媒

実験手順

Pyridine (0.16 ml) and benzyloxyacetyl chloride (0.16 ml) were added to a solution of 3′-[{2-[4-(aminosulfonyl)phenyl]ethyl}aminomethyl]-N-[2-(1-pyrrolidinyl)ethyl]-[1,1′-biphenyl]-3-carboxamide (506 mg) in DMF (10 ml). The reaction mixture was stirred at room temperature for 16 hours, then diluted with water and extracted with ethyl acetate. The extract was washed with brine and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The residues were purified by silica gel column chromatography (dichloromethane/methanol=98/2), whereby the title compound (257 mg) was obtained.

後処理

  1. extractionextracted with ethyl acetate
  2. washThe extract was washed with brine
  3. dry with materialdried over anhydrous magnesium sulfate
  4. customthe solvent was evaporated under reduced pressure
  5. customThe residues were purified by silica gel column chromatography (dichloromethane/methanol=98/2), whereby the title compound (257 mg)
  6. customwas obtained

出典と根拠

ORDレコード
ord-d4cc21a4adb5481cb9c9581135c634cc
出典データセット
uspto-grants-2006_08
特許番号
US07091247B2

関連ノート

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