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Aza-Henry Route to PZQ

Published by MatTodd on 30 January 2006 - 11:12pm
Aza-Henry route to PZQ

We have designed a new synthesis of PZQ based on a catalytic, asymmetric aza-Henry reaction (Scheme 1). The key step is the generation of the new stereogenic centre in 4. From here, the reduction to 5 should be facile with e.g. samarium iodide.1 From 5, the two steps to PZQ are known from the original report.2

Enantioselective Synthesis of Praziquantel

Published by ndt228 on 30 January 2006 - 11:06pm


  1. To develop an efficient enantioselective synthesis of the bioactive enantiomer of Praziquantel
  2. To optimize such a synthesis so it is suitable for large-scale manufacture.