710299-11-9Relevant academic research and scientific papers
Synthesis of [O-methyl-11C]1-(2-chlorophenyl)-5-(4- methoxyphenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide: A potential PET ligand for CB1 receptors
Kumar, J.S. Dileep,Prabhakaran, Jaya,Arango, Victoria,Parsey, Ramin V.,Underwood, Mark D.,Simpson, Norman R.,Kassir, Suham A.,Majo, Vattoly J.,Van Heertum, Ronald L.,Mann, J. John
, p. 2393 - 2396 (2004)
Synthesis and in vitro evaluation of [O-methyl-11C]1-(2- chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide ([11C]-1), a potential imaging agent for CB 1 receptors using PET is described. 1-(2-Chlorophenyl)-5-(4- hydroxyphenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (5), the precursor for radiolabeling, was synthesized from 4-OTBDPS-propiophenone (2) in five steps with 30% overall yield. The reaction of alcohol 5 with [ 11C]MeOTf at 60°C afforded [11C]-1 with an average radiochemical yield of 14.5% (EOS) and >2000Ci/mmol specific activity. The radiotracer was found to selectively label CB1 receptors in slide-mounted sections of postmortem human brain containing prefrontal cortex as demonstrated by in vitro autoradiography using phosphor imaging.
