Yinsheng Zhang
Sep 1, 2012
Citations
0
Influential Citations
2
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
4-[1-Methyl-2,4-dioxo-6-(3-phenyl-prop-1-ynyl)-1,4-dihydro-2H-quinazolin-3-ylmethyl]-benzoic acid, PD0331179, was under investigation as a matrix metalloproteinase-13 inhibitor. 14C-labeled and 2H-labeled PD0331179 and its 2H-labeled metabolite (PD0335699) were required to support its preclinical and clinical studies. [14C] 3-phenyl-1-trimethyl/triphenylsilyl-propyne was efficiently prepared starting with [14C] benzoic acid and used as a key-labeled reagent for the synthesis of [14C] PD0331179. A one-pot coupling reaction between aryl iodide and trialkylsilyl propyne was developed to make this synthesis more efficient. The details of these syntheses are reported. Copyright © 2012 John Wiley & Sons, Ltd.