反应 #1269890

反应方程式

triacetoxyborohydride

5-Amino-2-butylisoindolin-1-one

4-(benzylamino)nicotinaldehyde

NaHCO3

Sodium triacetoxyborohydride

→

5-((4-(benzylamino)pyridin-3-yl)methylamino)-2-butylisoindolin-1-one

收率 16.9%

溶剂

water

acetic acid

反应条件

后处理

1. 1
   workup.STIRRINGstirring for 6 h
2. 2
   workup.ADDITIONwere added
3. 3
   萃取The mixture was extracted with EtOAc
4. 4
   洗涤layers washed with water
5. 5
   干燥dried (MgSO4)
6. 6
   其他Purification by HPLC

实验过程

5-Amino-2-butylisoindolin-1-one (48.1 mg, 0.236 mmol) was added to a solution of 4-(benzylamino)nicotinaldehyde (50 mg, 0.236 mmol) in acetic acid (0.5 mL). Sodium triacetoxyborohydride (100 mg, 0.471 mmol) was added and the reaction mixture was stirred for 2 days. After the addition of more triacetoxyborohydride (50 mg, 0.235 mmol) and stirring for 6 h, water and sat aqueous NaHCO3 solution were added. The mixture was extracted with EtOAc, the combined org. layers washed with water and dried (MgSO4). Purification by HPLC provided 5-((4-(benzylamino)pyridin-3-yl)methylamino)-2-butylisoindolin-1-one (16 mg, 13%). ESI-MS [M+H+]=401.2.

来源