反応式
[Cl:1][C:2]1[C:10]2[C:5](=[CH:6][CH:7]=[CH:8][C:9]=2[NH2:11])[N:4]([CH2:12][CH2:13][N:14]2[CH2:18][CH2:17][CH2:16][CH2:15]2)[N:3]=1.[CH2:19]([O:26][C:27]1[CH:32]=[CH:31][C:30]([CH2:33][C:34](O)=[O:35])=[CH:29][CH:28]=1)[C:20]1[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=1.Cl.C(N=C=NC(C)(C)CC)C.ON1C2C=CC=CC=2N=N1.CN1CCOCC1>CN(C=O)C>[CH2:19]([O:26][C:27]1[CH:28]=[CH:29][C:30]([CH2:33][C:34]([NH:11][C:9]2[CH:8]=[CH:7][CH:6]=[C:5]3[C:10]=2[C:2]([Cl:1])=[N:3][N:4]3[CH2:12][CH2:13][N:14]2[CH2:18][CH2:17][CH2:16][CH2:15]2)=[O:35])=[CH:31][CH:32]=1)[C:20]1[CH:21]=[CH:22][CH:23]=[CH:24][CH:25]=1参加物
7
反応物 5
生成物 1
試薬・触媒・溶媒 1
実験手順
A mixture of 3-chloro-1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-4-ylamine (300 mg, 1.14 mmol), (4-benzyloxy-phenyl)-acetic acid (302 mg, 1.25 mmol), ethyldimethylpropylcarbodiimide hydrochloride (261 mg g, 1.37 mmol), N-hydroxybenzotriazole (184 mg, 1.37 mmol), N-methyl morpholine (290 mg, 2.72 mmol) in 5 mL of DMF was stirred for 6 hours and concentrated under reduced pressure. The residue was purified by flash chromatography (silica gel, triethylamine/ethyl acetate, 1/10) to provide the title compound. 1H NMR (300 MHz, DMSO-d6) ppm 1.60 (m, 4H), 2.43 (m, 4H), 2.85 (t, 2H, J=6.44), 3.69 (s, 2H), 4.48 (t, 2H, J=6.44), 5.10 (s, 2H), 6.99 (d, 2H, J=8.81), 7.28–7.48 (m, 9H), 7.59 (m, 1H), 10.10 (s, 1H); MS (DCI/NH3) m/z 489 [M+H]+.
後処理
- concentrationconcentrated under reduced pressure
- customThe residue was purified by flash chromatography (silica gel, triethylamine/ethyl acetate, 1/10)
出典と根拠
- ORDレコード
- ord-4e118547db8643f1873744afbd99b347
- 出典データセット
- uspto-grants-2006_07
- 特許番号
- US07071182B2
関連ノート
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