Реакция #86200

Уравнение реакции

water

1-[6-chloro-5-(trifluoromethyl)-2-pyridyl]-6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridine

tert-butyl N-[(3S)-3-piperidyl]carbamate

N-Methylmorpholine

→

tert-butyl N-[(3S)-1-[6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-3-(trifluoromethyl)-2-pyridyl]-3-piperidyl]carbamate

Выход 76.2%

Растворители

1-methyl-2-pyrrolidinone

Условия реакции

Обработка

1. 1
   Экстракцияextracted with EtOAc
2. 2
   КонцентрированиеThe organic layer was concentrated
3. 3
   ДругоеThe residue was purified on silica
4. 4
   Промывкаeluted with 0 to 100% EtOAc in Heptane

Методика

A mixture of 1-[6-chloro-5-(trifluoromethyl)-2-pyridyl]-6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridine (0.0876 mmol; 59.7 mg), tert-butyl N-[(3S)-3-piperidyl]carbamate (0.263 mmol; 52.6 mg), and N-Methylmorpholine (0.263 mmol; 26.9 mg; 0.0292 mL) in 1-methyl-2-pyrrolidinone (3 mL) in a sealed pressure vial was heated at 120° C. overnight. The mixture was poured into water, and extracted with EtOAc. The organic layer was concentrated. The residue was purified on silica eluted with 0 to 100% EtOAc in Heptane to afford tert-butyl N-[(3S)-1-[6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-3-(trifluoromethyl)-2-pyridyl]-3-piperidyl]carbamate as a white solid (37.0 mg, 65%).

Источник