反応 #73032

反応方程式

Trimethylorthobutyrate

4-[(3-amino[1,5]naphthyridin-4-ylamino)methyl]tetrahydropyran-4-ol

→

4-[(2-propyl-1H-imidazo[4,5-c][1,5]naphthyridin-1-yl)methyl]tetrahydro-2H-pyran-4-ol

収率 69.2%

溶媒

toluene

反応条件

後処理

1. 1
   温度The reaction mixture was heated
2. 2
   温度at reflux overnight
3. 3
   濃縮concentrated under reduced pressure
4. 4
   その他The residue was triturated with acetonitrile
5. 5
   その他the resulting solid was isolated by filtration

実験手順

Trimethylorthobutyrate (1.9 mL, 12.0 mmol) and pyridine hydrochloride (23 mg, 0.2 mmol) were added to a suspension of 4-[(3-amino[1,5]naphthyridin-4-ylamino)methyl]tetrahydropyran-4-ol (10.0 mmol) in toluene (50 mL). The reaction mixture was heated at reflux overnight and then concentrated under reduced pressure. The residue was triturated with acetonitrile and the resulting solid was isolated by filtration to provide 2.26 g of 4-[(2-propyl-1H-imidazo[4,5-c][1,5]naphthyridin-1-yl)methyl]tetrahydro-2H-pyran-4-ol as a tan solid.

出典