Racemic Resolution of Praziquantel and Praziquanamine

 

Hazard and Risk Assessment:

To a cooled solution of MNR27-1 ( mmol) in DCM (5 mL) at 0°C was added triethylamine (0.21 mL, mol) and benzoyl chloride(0.13 mL, 1.09 mmol). The solution was stirred overnight at room temperature.

The solution was quenched with water (5 mL) and stirred for a further 30 min. The layers were separated and the organic layer was washed with saturated sodium carbonate solution (5 mL), 0.5 M HCl (5 mL) and brine (5 mL). Dried over magnesium sulfate, filtered and concentrated under reduced pressure to give the crude as an orange oil (0.240 g).

Column:- 50-100 EtOAc/PetEther

Fracs 15-24 0.121 g, 0.33 mmol, 67% yield

Melting point 94-95 °C