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17th June 2010 @ 07:55
Preparation of starting material for the Ugi reaction(MeO)2-derivative of PZQ

Hazard and Risk Assessment:
Reaction Class: 2
Hazards: T Toxic, X Irritant, C Corrosive
Risk rating: U = Unlikely

Start time: 4:50 PM 17/06/2010
End time: --

To a mixture of 3,4-dimethoxyphenethylamine (1.00 g, 5.52 mmol), benzyltriethylammonium chloride (TEBACl) (64 mg, 276 µmol, 5 mol%) and NaOH (442 mg, 11.0 mmol, 2 eq.) in CH2Cl2 (20 mL) was added chloroform (1.0 g, 0.67 mL, 8.79 mmol, 1.5 eq.) and heated to reflux.


References:
[1] “Novel Synthesis of Praziquantel“, A. Dömling, Patent Application 2009, WO 2009/11533(A1), Language: German.

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