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Studies on the dynamic resolution of Crizotinib intermediate.

Alexandre da S de França1, Marcus V M Silva1, Rebeca V Neves1

  • 1Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.

Bioorganic & Medicinal Chemistry
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Summary

Researchers explored biocatalytic methods for synthesizing a key chiral intermediate for Crizotinib, an anti-cancer drug. Both kinetic and dynamic resolutions achieved high selectivity and conversion, optimizing production of this vital compound.

Keywords:
Continuous-flowCrizotinibDynamic resolutionKinetic resolutionLipases

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Area of Science:

  • Organic Chemistry
  • Biocatalysis
  • Pharmaceutical Synthesis

Background:

  • Crizotinib is a crucial anti-cancer agent for non-small cell lung carcinoma treatment.
  • Efficient synthesis of its chiral intermediate, 1-(2,6-dichloro-3-fluorophenyl)ethanol, is essential for drug production.
  • Biocatalytic approaches offer promising routes for producing chiral intermediates.

Purpose of the Study:

  • To investigate kinetic and dynamic resolution methods for the chiral intermediate of Crizotinib.
  • To evaluate the efficiency and selectivity of biocatalytic strategies for this synthesis.
  • To optimize the production of the desired chiral intermediate for Crizotinib.

Main Methods:

  • Employed kinetic resolution to selectively produce the desired enantiomer of 1-(2,6-dichloro-3-fluorophenyl)ethanol.
  • Utilized dynamic kinetic resolution under continuous-flow conditions for enhanced intermediate production.
  • Analyzed conversion rates and enantiomeric excess (e.e.) to assess method efficacy.

Main Results:

  • Kinetic resolution achieved high selectivity with an enantiomeric ratio (E) greater than 200 at 45% conversion.
  • Dynamic kinetic resolution under continuous-flow conditions yielded the desired product with 57% conversion and 98% e.e.
  • Both methods demonstrate significant potential for efficient chiral intermediate synthesis.

Conclusions:

  • Biocatalytic kinetic and dynamic resolutions are effective strategies for producing the chiral intermediate of Crizotinib.
  • Continuous-flow dynamic kinetic resolution offers a highly efficient route with excellent enantioselectivity.
  • These optimized methods contribute to the scalable and sustainable synthesis of Crizotinib.