تفاعل #1269889

معادلة التفاعل

5-amino-2-butylisoindolin-1-one

4-(trifluoromethyl)nicotinaldehyde

water

→

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

المردود 19.0%

المذيبات

MeOH

ظروف التفاعل

المعالجة

1. 1
   workup.ADDITIONwas added
2. 2
   استخلاصThe reaction mixture was extracted with EtOAc
3. 3
   غسيلlayers were washed with water
4. 4
   تجفيفdried (MgSO4)
5. 5
   أخرىthe solvent was removed in vacuo
6. 6
   أخرىPurification by HPLC

الإجراء التجريبي

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.

المصدر