60725-35-1Relevant articles and documents
Syntheses of [14C] and [2H4]PD0205520, an inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor
Zhang, Yinsheng,Huang, Yun,Huang, Che C.
, p. 485 - 496 (2007/10/03)
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 14C-labeled in the pyrimidine ring system was prepared in seven steps in an overall radiochemical yield of 26% from [14C]thiourea. PD0205520 2H-labeled in the piperazine ring was synthesized in four steps in a 32% overall yield. Copyright
