Reacción #86121

Ecuación de reacción

2-bromo-6-fluoropyridine

tert-butyl 1,4-diazepane-1-carboxylate

DIPEA

→

tert-butyl 4-(6-bromopyridin-2-yl)-1,4-diazepane-1-carboxylate

Rendimiento 50.1%

Disolventes

ethanol

Condiciones de reacción

Tratamiento posterior

1. 1
   ConcentraciónThe reaction mixture was concentrated under reduced pressure
2. 2
   workup.ADDITIONthe residue was diluted with EtOAc (100 mL)
3. 3
   LavadoThe solution was washed with brine
4. 4
   Secadodried over Na2SO4
5. 5
   Concentraciónconcentrated under reduced pressure

Procedimiento

A mixture of 2-bromo-6-fluoropyridine (500 mg, 2.8 mmol), tert-butyl 1,4-diazepane-1-carboxylate (568 mg, 2.8 mmol) in DIPEA (1.83 g, 14.2 mmol) in ethanol (10 mL) was heated at 100° C. for 16 hours. The reaction mixture was concentrated under reduced pressure and the residue was diluted with EtOAc (100 mL). The solution was washed with brine, dried over Na2SO4, and concentrated under reduced pressure to afford tert-butyl 4-(6-bromopyridin-2-yl)-1,4-diazepane-1-carboxylate as a colorless oil (500 mg, 50%). MS (ESI) m/z: 356 [M+H]+.

Fuente