Enantioselective Hydrogenation of dehydro-PZQ and derivatives

 

Hazard and Risk Assessment:


Procedure:
A mixture of rac-PZQ (1.0 g, 3.2 mmol) and sulfur (0.210 g, 6.4 mmol) under argon was heated at 190°C for 15 minutes by use of a heat gun. The dark brown solid was dissolved in ethyl acetate, evaporated on silica gel and purified by column chromatography (20-40% EtoAC/Hex)

Frac 17-30 - 0.455 g, 1.46 mmol, 46 % as a yellow solid

Frac 40-44 - 0.328 g, 1.05 mmol, 33 % recovered PZQ

1 H NMR
13C NMR

FCC fractions ran in 50% EtOAC/Hexane