Diisobutylamine → {2-[5-diisobutylcarbamoyl-2-(3,5-dimethylphenyl)-1H-indol-3-yl]-ethyl}carbamic acid tert-butyl ester

HRID 1458360ノート

反応式

HRID 1458360 の反応式
[C:1]([O:5][C:6]([NH:8][CH2:9][CH2:10][C:11]1[C:19]2[C:14](=[CH:15][CH:16]=[C:17]([C:20]([OH:22])=O)[CH:18]=2)[NH:13][C:12]=1[C:23]1[CH:28]=[C:27]([CH3:29])[CH:26]=[C:25]([CH3:30])[CH:24]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].ON1C2C=CC=CC=2N=N1.Cl.CN(C)CCCN=C=NCC.[CH2:53]([NH:57][CH2:58][CH:59]([CH3:61])[CH3:60])[CH:54]([CH3:56])[CH3:55]>>[C:1]([O:5][C:6](=[O:7])[NH:8][CH2:9][CH2:10][C:11]1[C:19]2[C:14](=[CH:15][CH:16]=[C:17]([C:20](=[O:22])[N:57]([CH2:58][CH:59]([CH3:61])[CH3:60])[CH2:53][CH:54]([CH3:56])[CH3:55])[CH:18]=2)[NH:13][C:12]=1[C:23]1[CH:28]=[C:27]([CH3:29])[CH:26]=[C:25]([CH3:30])[CH:24]=1)([CH3:2])([CH3:3])[CH3:4]

参加物

5

実験手順

To a solution of 3-(2-tert-butoxycarbonylaminoethyl)-2-(3,5-dimethylphenyl)-1H-indole-5-carboxylic acid (200 mg in 12 mL methylene chloride) was added 104 mg 1-hydroxybenzotriazole followed by 118 mg 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and the mixture stirred at room temperature. After 30 minutes, 0.35 mL of diisobutylamine was added and the mixture stirred at room temperature for 14 hours. The reaction was then concentrated in vacuo and purified by flash chromatography on silica gel (hexane:ethyl acetate, 2:1) to give the title compound (230 mg).

後処理

  1. stirringthe mixture stirred at room temperature for 14 hours
  2. concentrationThe reaction was then concentrated in vacuo
  3. custompurified by flash chromatography on silica gel (hexane:ethyl acetate, 2:1)

出典と根拠

ORDレコード
ord-22d888a44b0b4c7fb739c3fa3d75a7ca
出典データセット
uspto-grants-1998_12
特許番号
US05849764

反応ノート

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