title: A general method for the synthesis of aryl [11C]methylsulfones: potential PET probes for imaging cyclooxygenase-2 expression.
abstract: A general one-pot method has been developed for the conversion of an aryl thiol moiety masked as the butyrate ester to the corresponding 11C-labeled methylsulfone group. The potential of this methodology has been demonstrated by the successful radiosynthesis of carbon-11 analogues of several highly selective cyclooxygenase-2 (COX-2) inhibitors such as Rofecoxib, Etoricoxib, and 3-(4-methylsulfonylphenyl)-4-phenyl-5-trifluoromethyl isoxazole in high yield. The chemical and radiochemical purities obtained for the 11C-labeled COX-2 inhibitors are >99% with a specific activity >1000 Ci/mmol.
authors.affiliation: Department of Psychiatry, New York State Psychiatric Institute, New York, NY 10032, USA.
authors.forename: Vattoly J
authors.initials: VJ
authors.lastname: Majo
authors.forename: Jaya
authors.initials: J
authors.lastname: Prabhakaran
authors.forename: Norman R
authors.initials: NR
authors.lastname: Simpson
authors.forename: Ronald L
authors.initials: RL
authors.lastname: Van Heertum
authors.forename: J John
authors.initials: JJ
authors.lastname: Mann
authors.forename: J S Dileep
authors.initials: JS
authors.lastname: Kumar
mesh_terms: D002250:Carbon Radioisotopes; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry; D008722:Methods; D008745:Methylation; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis*
chemical_list: D002250:Carbon Radioisotopes; D016861:Cyclooxygenase Inhibitors; D019275:Radiopharmaceuticals; D013450:Sulfones