反应 #328804

反应方程式

trifluoroacetic acid

4-(1-(4-Methoxyphenyl)-3-(methylthio)-1H-indol-2-yl)-3,5-dimethylisoxazole

2-mercaptobenzoic acid

NaOH

→

4-(1-(4-methoxyphenyl)-1H-indol-2-yl)-3,5-dimethylisoxazole

收率 86.0%

反应条件

后处理

1. 1
   其他the phases were separated
2. 2
   其他The solvents were evaporated
3. 3
   其他the residue was purified by flash chromatography with heptane/EtAc 4:1 as eluent

实验过程

4-(1-(4-Methoxyphenyl)-3-(methylthio)-1H-indol-2-yl)-3,5-dimethylisoxazole (the intermediate product of step (c) from the synthesis of Example 21, 140 mg, 0.38 mmol) and 2-mercaptobenzoic acid (118 mg, 0.77 mmol) were added to 5 ml of trifluoroacetic acid at RT. The mixture was stirred as a slurry at RT under an atmosphere of nitrogen over night. 2M NaOH and EtAc were added and the phases were separated. The solvents were evaporated and the residue was purified by flash chromatography with heptane/EtAc 4:1 as eluent to provide 4-(1-(4-methoxyphenyl)-1H-indol-2-yl)-3,5-dimethylisoxazole in 86% yield. ES/MS m/z: 319.1 (M+H)

来源