Cyclopentanecarboxylic acid → N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]cyclopentanecarboxamide

HRID 13058

反応式

HRID 13058 の反応式
[CH:1]1([C:6]([OH:8])=O)[CH2:5][CH2:4][CH2:3][CH2:2]1.[F:9][C:10]1[CH:15]=[CH:14][C:13]([N:16]2[C:24]3[C:19](=[CH:20][C:21]([O:25][C@H:26]([C:30]4[CH:35]=[CH:34][CH:33]=[C:32]([O:36][CH3:37])[CH:31]=4)[C@@H:27]([NH2:29])[CH3:28])=[CH:22][CH:23]=3)[CH:18]=[N:17]2)=[CH:12][CH:11]=1>ClCCl>[F:9][C:10]1[CH:11]=[CH:12][C:13]([N:16]2[C:24]3[C:19](=[CH:20][C:21]([O:25][C@H:26]([C:30]4[CH:35]=[CH:34][CH:33]=[C:32]([O:36][CH3:37])[CH:31]=4)[C@@H:27]([NH:29][C:6]([CH:1]4[CH2:2][CH2:3][CH2:4][CH2:5]4)=[O:8])[CH3:28])=[CH:22][CH:23]=3)[CH:18]=[N:17]2)=[CH:14][CH:15]=1

参加物

4

反応物 2

HCID 18840Cyclopentanecarboxylic acidHCID 59339733(1R,2S)-1-(1-(4-fluorophenyl)indazol-5-yloxy)-1-(3-methoxyphenyl)propan-2-amine

生成物 1

HCID 25012194N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]cyclopentanecarboxamide

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒2 回

実験手順

To a stirred solution of 1,1-carbonyldiimidazole (12 mg, 70 μmol) in dichloromethane (1 ml) was added cyclopentanecarboxylic acid (11 μl, 100 μmol) to give a colorless solution. The reaction mixture was stirred for 1 h at r.t. Then a solution of (1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-(3-methoxyphenyl)propan-2-amine (6a, 19 mg, 50 μmol) in dichloromethane (0.5 ml) was added, and the stirring was continued at r.t. overnight. The solvent was removed in vacuo, the residue dissolved in acetonitrile/water mixture, and the crude product purified by preparative HPLC. Yield 18 mg (76%).

後処理

  1. customto give a colorless solution
  2. waitthe stirring was continued at r.t. overnight
  3. customThe solvent was removed in vacuo
  4. dissolutionthe residue dissolved in acetonitrile/water mixture
  5. customthe crude product purified by preparative HPLC

出典と根拠

ORDレコード
ord-105ac68a9d904dd4bcd2b0ac87f84a82
出典データセット
uspto-grants-2010_06
特許番号
US07728030B2

関連ノート

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