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Syntheses of [14C] and [2H4]PD0205520, an inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor

✍ Scribed by Yinsheng Zhang; Yun Huang; Che C. Huang

Publisher: John Wiley and Sons
Year: 2005
Tongue: French
Weight: 142 KB
Volume: 48
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.944

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✦ Synopsis

Abstract

5‐(4‐Methyl‐piperazin‐1‐yl)‐pent‐2‐ynoic acid [4‐(3‐chloro‐4‐fluoro‐phenylamino)‐pyrido[3,4‐d]pyrimidin‐6‐yl]‐amide, PD0205520, was under investigation as a potential inhibitor of the tyrosine kinase (TK) activity of the epidermal growth factor receptor (EGFR) for cancer treatment. Both radio‐ and stable‐isotope‐labeled compounds were required for drug absorption, distribution, metabolism and excretion (ADME) and quantitative mass spectrometry bio‐analytical studies. PD0205520 ^I4^C‐labeled in the pyrimidine ring system was prepared in seven steps in an overall radiochemical yield of 26% from [^14^C]thiourea. PD0205520 ^2^H‐Iabeled in the piperazine ring was synthesized in four steps in a 32% overall yield. Copyright © 2005 John Wiley & Sons, Ltd.

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