تفاعل #86155

معادلة التفاعل

2-bromo-6-fluoropyridine

tert-butyl 6-methylpiperidin-3-ylcarbamate

→

tert-butyl N-[1-(6-bromo-2-pyridyl)-6-methyl-3-piperidyl]carbamate

المردود 39.0%

المذيبات

methyl sulfoxide

ظروف التفاعل

المعالجة

1. 1
   أخرى18 h
2. 2
   أخرىThe reaction was quenched with water
3. 3
   استخلاصthen extracted with EtOAc
4. 4
   تجفيفThe organic layers was dried with sodium sulfate
5. 5
   ترشيحfiltered
6. 6
   تركيزconcentrated in vacuum
7. 7
   أخرىThe crude product was purified by flash chromatography (EtOAc/Heptane eluted at 30% EtOAc)

الإجراء التجريبي

A solution containing 2-bromo-6-fluoropyridine (0.95 mL, 6.65 mmol and tert-butyl 6-methylpiperidin-3-ylcarbamate (750 mg, 3.32 mmol) in methyl sulfoxide 5.0 ml was heated 95° C. 18 h. The reaction was quenched with water then extracted with EtOAc. The organic layers was dried with sodium sulfate, filtered, and concentrated in vacuum. The crude product was purified by flash chromatography (EtOAc/Heptane eluted at 30% EtOAc) to give tert-butyl N-[1-(6-bromo-2-pyridyl)-6-methyl-3-piperidyl]carbamate (480 mg) in 39% yield. MS (ESI) m/z: 371.2

المصدر