Resolution of Praziquantel
2011

New Methods for Producing Praziquantel as a Single Enantiomer

publication Evidence: moderate

Author Information

Author(s): Michael Woelfle, Jean-Paul Seerden, Jesse de Gooijer, Kees Pouwer, Piero Olliaro, Matthew H. Todd

Primary Institution: School of Chemistry, The University of Sydney

Hypothesis

Can enantiopure praziquantel be obtained without a significant increase in price?

Conclusion

Both resolution procedures identified show promise for the large-scale, economically viable production of praziquantel as a single enantiomer for a low price.

Supporting Evidence

  • Praziquantel is the main drug used to treat schistosomiasis.
  • The inactive enantiomer of praziquantel causes side effects and a bitter taste.
  • Open collaboration led to the discovery of new methods for producing praziquantel.
  • Both methods can produce enantiopure praziquantel economically.
  • Smaller quantities of the drug can be produced for research purposes.

Takeaway

Researchers found two ways to make praziquantel, a medicine for schistosomiasis, in a purer form that is cheaper and easier to use.

Methodology

Two resolution approaches were identified: one through hydrolysis of praziquantel and another using a different intermediate resolved with tartaric acid.

Limitations

The methods may not be suitable for all laboratories due to the need for specific conditions and materials.

Digital Object Identifier (DOI)

10.1371/journal.pntd.0001260

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