Реакция #86121

Уравнение реакции

2-bromo-6-fluoropyridine

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

DIPEA

→

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

Выход 50.1%

Растворители

ethanol

Условия реакции

Обработка

1. 1
   КонцентрированиеThe reaction mixture was concentrated under reduced pressure
2. 2
   workup.ADDITIONthe residue was diluted with EtOAc (100 mL)
3. 3
   ПромывкаThe solution was washed with brine
4. 4
   Сушкаdried over Na2SO4
5. 5
   Концентрированиеconcentrated under reduced pressure

Методика

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]+.

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