Реакция #2366787

Уравнение реакции

426

trans-(±)-3-azido-4-(4-chloro-3-fluorophenoxy)-1-methylpyrrolidine

PPh3

THF

→

trans-(±)-4-(4-chloro-3-fluorophenoxy)-1-methylpyrrolidin-3-amine

Выход 21.0%

Растворители

H2O

Условия реакции

Обработка

1. 1
   ДругоеThe solvent was removed in vacuo
2. 2
   ДругоеThe residue was purified by SiO2 chromatography
3. 3
   Промывкаeluting with DCM/MeOH (5:1 DCM/MeOH

Методика

To a solution of 426 (0.480 g, 1.77 mmol), PPh3 (0.930 g, 3.54 mmol) and THF (10 mL) was added H2O (1.0 mL). The resultant mixture was heated at 55° C. for 3 h. The solvent was removed in vacuo. The residue was purified by SiO2 chromatography eluting with DCM/MeOH (5:1 DCM/MeOH then 1:1) to afford 85 mg (21% over 5 steps) of trans-(±)-4-(4-chloro-3-fluorophenoxy)-1-methylpyrrolidin-3-amine (428): LC-MS (ESI) m/z 245 (M+H).

Источник