反应 #1269889

反应方程式

5-amino-2-butylisoindolin-1-one

4-(trifluoromethyl)nicotinaldehyde

water

→

2-butyl-5-((4-(trifluoromethyl)pyridin-3-yl)methylamino)isoindolin-1-one TFA

收率 19.0%

溶剂

MeOH

反应条件

后处理

1. 1
   workup.ADDITIONwas added
2. 2
   萃取The reaction mixture was extracted with EtOAc
3. 3
   洗涤layers were washed with water
4. 4
   干燥dried (MgSO4)
5. 5
   其他the solvent was removed in vacuo
6. 6
   其他Purification by HPLC

实验过程

5-amino-2-butylisoindolin-1-one (35.0 mg, 0.17 mmol), ZnCl2 (14.0 mg, 0.10 mmol) and NaCNBH4 (12.9 mg, 0.21 mmol) were consecutively added to a solution of 4-(trifluoromethyl)nicotinaldehyde (30.0 mg, 0.17 mmol) in MeOH (4 mL). After stirring overnight at room temperature excess water was added. The reaction mixture was extracted with EtOAc, the combined org. layers were washed with water, dried (MgSO4) and the solvent was removed in vacuo. Purification by HPLC provided 2-butyl-5-((4-(trifluoromethyl)pyridin-3-yl)methylamino)isoindolin-1-one TFA (16.0 mg, 19%). ESI-MS [M+H]+=364.2.

来源