反応 #69150

反応方程式

4-(5-methyl-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2-(methylsulfonyl)pyrimidine-5-carbonitrile

(R)-(−)-2-amino-3-methyl-1-butanol

diisopropylethylamine

→

title compound

収率 77.0%

2-((R)-1-hydroxy-3-methylbutan-2-ylamino)-4-(5-methyl-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidine-5-carbonitrile

収率 77.0%

溶媒

THF

反応条件

後処理

1. 1
   温度was heated
2. 2
   温度at reflux for 1 hour
3. 3
   濃縮The reaction mixture was concentrated in vacuo
4. 4
   その他the residue was purified on silica gel by flash column chromatography

実験手順

A mixture of 4-(5-methyl-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2-(methylsulfonyl)pyrimidine-5-carbonitrile (120 mg, 0.257 mmol), (R)-(−)-2-amino-3-methyl-1-butanol (57 μl, 0.515 mmol) and diisopropylethylamine (90 μl, 0.515 mmol) in THF (4 mL) was heated at reflux for 1 hour. The reaction mixture was concentrated in vacuo and the residue was purified on silica gel by flash column chromatography to give the title compound as a colourless glassy solid (97 mg, 77% yield).

出典