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Attrition-Enhanced Deracemization in the Synthesis of Clopidogrel - A Practical Application of a New Discovery

Meijden, M. W. V. D., Leeman, M., Gelens, E., Noorduin, W. L., Meekes, H., Enckevort, W. J. P. V., Kaptein, B., Vlieg, E. & Kellogg, R. M., 2009, In : Organic Process Research & Development. 13, 6, p. 1195-1198 4 p.

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DOI

  • Maarten W. van der Meijden
  • Michel Leeman
  • Edith Gelens
  • Wim L. Noorduin
  • Hugo Meekes
  • Willem J.P. van Enckevort
  • Bernard Kaptein
  • Elias Vlieg
  • Richard M. Kellogg
The recently discovered technique of deracemization by means of attrition-induced grinding of a solid conglomerate in contact with a solution wherein racemization occurs has been used with a derivative of 2-chlorophenyl glycine, the key chiral component in the synthesis of Clopidogrel (Plavix). Deracemization of the racemate proceeds to a single enantiomer and in essentially absolute enantiomeric excess. Further conversion of enantiomerically pure material to Clopidogrel was achieved in 88% yield.
Original languageEnglish
Pages (from-to)1195-1198
Number of pages4
JournalOrganic Process Research & Development
Volume13
Issue number6
Publication statusPublished - 2009

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