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

✍ Scribed by Tony Taldone; Danuta Zatorska; Yanlong Kang; Gabriela Chiosis

• Book ID: 102367503
• Publisher: John Wiley and Sons
• Year: 2009
• Tongue: French
• Weight: 146 KB
• Volume: 53
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.1689

✦ Synopsis

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 d~6~‐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‐d~6~ was synthesized in five steps using readily available 1,3‐dibromopropane‐d~6~ and is an important compound for the advancement of our clinical program. Copyright © 2009 John Wiley & Sons, Ltd.