反応 #3484

反応方程式

Methyl bromoacetate

4-Amino-2-Ethyl-α-oxo-1-(phenylmethyl)-1H-indole-3-Acetamide

→

[[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]amino]acetic acid methyl ester

収率 64.0%

溶媒

water

DMF

反応条件

後処理

1. 1
   workup.WAITat room temperature for 20 hours
2. 2
   抽出extracted with EtOAc
3. 3
   洗浄The EtOAC solution was washed with brine
4. 4
   乾燥dried over MgSO4
5. 5
   その他evaporated in vacuo
6. 6
   その他The residue was chromatographed over silica gel eluting with Hexane/50 to 100% EtOAc

実験手順

Methyl bromoacetate (0.07 ml, 0.78 mmol) was added to 250 mg (0.78 mmol) of 4-Amino-2-Ethyl-α-oxo-1-(phenylmethyl)-1H-indole-3-Acetamide in 4 ml of DMF, stirred at 60° C. for 0.5 hour, and then at room temperature for 20 hours. The mixture was diluted with water and extracted with EtOAc. The EtOAC solution was washed with brine, dried over MgSO4, and evaporated in vacuo. The residue was chromatographed over silica gel eluting with Hexane/50 to 100% EtOAc to give 196 mg (64%) of [[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]amino]acetic acid methyl ester melting at 188°-193° C.

出典