反应详情

tert-butyl-4-amino-3-hydroxypiperidine-1-carboxylate (11.9 g; 55 mmol) and benzophenone imine (10 g; 59 mmol; 1.05 eq.) were dissolved in anhydrous toluene and heated to reflux for 18 hrs. Monitored the reaction by TLC (30% EtOAc/hexanes with 0.1% triethylamine). The crude reaction was concentrated and purified by flash column chromatography. Isolation gave 18.4 g of the title compound in an 86% yield. LC/MS (ES+)[(M+H)+]: 381 for C23H28N2O3.

1. temperatureheated
2. temperatureto reflux for 18 hrs
3. customThe crude reaction
4. concentrationwas concentrated
5. custompurified by flash column chromatography