反応 #89703

反応方程式

diisopropylethylamine

piperidine-2,3-dicarboxylic acid 3-tert-butyl ester

4-(3-isopropyl-phenyl)-1,2,3,6-tetrahydropyridine

PyBOP

→

4-(3-Isopropyl-phenyl-3,6-dihydro-2H-pyridine-1-carbonyl]-piperidine-3-carboxylic acid tert-butyl ester

溶媒

EtOAc

DMF

反応条件

後処理

1. 1
   洗浄washed with saturated NaHCO3 solution (×3), water, and brine
2. 2
   乾燥The organic layers were dried over MgSO4
3. 3
   ろ過filtered
4. 4
   濃縮concentrated
5. 5
   その他to dry under reduced pressure

実験手順

To a 0° C. solution of piperidine-2,3-dicarboxylic acid 3-tert-butyl ester (100 mg) in DMF (0.6 mL) was added sequentially, 4-(3-isopropyl-phenyl)-1,2,3,6-tetrahydropyridine (97 mg). PyBOP (232 mg), and diisopropylethylamine (0.152 mL). The resultant mixture was stirred at rt overnight. The reaction solution was diluted with EtOAc and washed with saturated NaHCO3 solution (×3), water, and brine. The organic layers were dried over MgSO4, filtered, and concentrated to dry under reduced pressure. The residue was used in next step without further purifications. MS (ESI): 413.2 (M+H+)

出典