反応 #47918

反応方程式

N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amine

p-tolylboronic acid

triethylamine

→

desired compound

収率 10.0%

N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydro-6-p-tolylpyrido[4,3-d]pyrimidin-4-amine

収率 10.0%

溶媒

THF

反応条件

後処理

1. 1
   その他the solvent was removed under a vacuum
2. 2
   その他The residue was purified

実験手順

N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amine (100 mg, 0.34 mmol) was dissolved in anhydrous THF (2 mL). To the mixture was added p-tolylboronic acid (92 mg, 0.68 mmol), Cu(OAc)2 (124 mg, 0.68 mmol) and triethylamine (0.68 g, 0.095 mL). The mixture was agitated for 6 h and the solvent was removed under a vacuum. The residue was purified using a gradient of ethyl acetate:hexane (0-100%) to give the desired compound as reddish powder (12.8 mg, 10%).

出典