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A facile and efficient synthesis of d 6 ‐labeled PU‐H71, a purine‐scaffold Hsp90 inhibitor
Author(s) -
Taldone Tony,
Zatorska Danuta,
Kang Yanlong,
Chiosis Gabriela
Publication year - 2010
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1689
Subject(s) - chemistry , hsp90 inhibitor , purine , combinatorial chemistry , scaffold , pharmacology , stereochemistry , biochemistry , enzyme , hsp90 , biomedical engineering , medicine , heat shock protein , gene
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.