Triethylamine → Methyl 4-(5-{(1R,2S)-2-[(2-furylcarbonyl)amino]-1-phenylpropoxy}-1H-indazole-1-yl)benzoate

HRID 1098903

反応式

HRID 1098903 の反応式
[NH2:1][C@@H:2]([CH3:30])[C@@H:3]([C:24]1[CH:29]=[CH:28][CH:27]=[CH:26][CH:25]=1)[O:4][C:5]1[CH:6]=[C:7]2[C:11](=[CH:12][CH:13]=1)[N:10]([C:14]1[CH:23]=[CH:22][C:17]([C:18]([O:20][CH3:21])=[O:19])=[CH:16][CH:15]=1)[N:9]=[CH:8]2.C(N(CC)CC)C.[O:38]1[CH:42]=[CH:41][CH:40]=[C:39]1[C:43](Cl)=[O:44]>ClCCl>[O:38]1[CH:42]=[CH:41][CH:40]=[C:39]1[C:43]([NH:1][C@@H:2]([CH3:30])[C@@H:3]([C:24]1[CH:25]=[CH:26][CH:27]=[CH:28][CH:29]=1)[O:4][C:5]1[CH:6]=[C:7]2[C:11](=[CH:12][CH:13]=1)[N:10]([C:14]1[CH:23]=[CH:22][C:17]([C:18]([O:20][CH3:21])=[O:19])=[CH:16][CH:15]=1)[N:9]=[CH:8]2)=[O:44]

参加物

5

反応物 3

HCID 8471TriethylamineHCID 682422-Furancarbonyl chlorideHCID 66812703Methyl 4-{5-[(1R,2S)-2-amino-1-phenylpropoxy]-1H-indazole-1-yl}benzoate

生成物 1

HCID 44515372Methyl 4-(5-{(1R,2S)-2-[(2-furylcarbonyl)amino]-1-phenylpropoxy}-1H-indazole-1-yl)benzoate収率 48.2%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒2 回

実験手順

Methyl 4-{5-[(1R,2S)-2-amino-1-phenylpropoxy]-1H-indazole-1-yl}benzoate (64.3 mg, 0.16 mmol) is dissolved in 6.1 mL of dichloromethane. Triethylamine (0.053 mL, 0.38 mmol) and 2-furoylchloride (20.9 mg, 0.16 mmol) are added. After 4 h stirring at r.t. the reaction mixture is diluted with dichloromethane, washed with water and brine and dried over Na2SO4. The reaction mixture is filtered, the solvent evaporated and the residue purified by chromatography (silicagel, eluents: ethyl acetate/hexane). 38.2 mg (48.1%) of the title compound are obtained.

後処理

  1. washwashed with water and brine
  2. dry with materialdried over Na2SO4
  3. filtrationThe reaction mixture is filtered
  4. customthe solvent evaporated
  5. customthe residue purified by chromatography (silicagel, eluents: ethyl acetate/hexane)

出典と根拠

ORDレコード
ord-d58368fb38d041339a22306bed43c8fa
出典データセット
uspto-grants-2012_03
特許番号
US08143290B2

関連ノート

読み込み中…