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Keywords:

  • deuterium labeled PU-H71;
  • purine;
  • heat shock protein 90;
  • inhibitor;
  • cancer

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.