Biotransformation-mediated synthesis of (1S)-1-(2,6-dichloro-3- fluorophenyl)ethanol in enantiomerically pure form

Carlos A. Martinez, Renzo Meijer, Gerard Metselaar, Gerlof Kruithof, Curtis Moore, Pei Pei Kung, Erik Keller

    Research output: Contribution to journalArticleAcademicpeer-review

    Abstract

    An efficient four-step biotransformation-mediated synthesis of (1S)-1-(2,6-dichloro-3-fluorophenyl)ethanol in enantiomerically pure form is described. This compound is a key intermediate required for the preparation of PF-2341066, a potent inhibitor of c-Met/ALK that is currently in clinical development. The described synthesis was used to manufacture 6 kg of the title compound and can also be employed to produce the corresponding (1R)-enantiomer. © 2010 Elsevier Ltd. All rights reserved.
    Original languageEnglish
    Pages (from-to)2408-2413
    JournalTetrahedron: asymmetry
    Volume21
    Issue number19
    DOIs
    Publication statusPublished - 7 Oct 2010

    Keywords

    • biotransformation
    • biocatalysis
    • PLE

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