A facile and efficient synthesis of d6-labeled PU-H71, a purine-scaffold Hsp90 inhibitor

Authors

  • Tony Taldone,

    1. Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY, USA
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  • Danuta Zatorska,

    1. Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY, USA
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  • Yanlong Kang,

    1. Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY, USA
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  • Gabriela Chiosis

    Corresponding author
    1. Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY, USA
    • Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, Box 482, New York, NY 10021, USA
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Abstract

PU-H71 is a purine-scaffold Hsp90 inhibitor currently undergoing late stage preclinical evaluation for the treatment of cancer. In this investigation, we present a simple method for the synthesis of d6-labeled PU-H71 for use as an internal standard to accurately quantitate the drug in biological matrices based on an LC-MS-MS method. PU-H71-d6 was synthesized in five steps using readily available 1,3-dibromopropane-d6 and is an important compound for the advancement of our clinical program. Copyright © 2009 John Wiley & Sons, Ltd.

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