title: A remote-controlled high pressure reactor for radiotracer synthesis with [11C]carbon monoxide.
abstract: [11C]Carbon monoxide is a versatile building block for the synthesis of PET radiotracers. However, the difficulty of trapping [11C]CO in a small solvent volume has limited its utility. We wish to report the details of a simple, remotely operated High Pressure Reactor (HiPR) system for trapping and reacting practical quantities of [11C]CO. All parts used in the HiPR are commercially available, providing an inexpensive and easily assembled system. A number of compounds have been synthesized using the HiPR via palladium mediated reactions with [11C]CO, an aryl halide, and a nucleophile dissolved in dioxane. For example, AMPA receptor modulator [11C]CX546 was synthesized from its respective precursors in 37% isolated yield, uncorrected from trapped [11C]CO.
authors.affiliation: Merck Research Laboratories, PO Box 4 WP44C-2, West Point, Pennsylvania 19486, USA. eric_hostetler@merck.com
authors.forename: Eric D
authors.initials: ED
authors.lastname: Hostetler
authors.forename: H Donald
authors.initials: HD
authors.lastname: Burns
mesh_terms: D002248:Carbon Monoxide / Q000138:chemical synthesis* / Q000302:isolation & purification; D002250:Carbon Radioisotopes / Q000737:chemistry* / Q000302:isolation & purification; D002851:Chromatography, High Pressure Liquid / Q000295:instrumentation* / Q000379:methods; D004149:Dioxoles / Q000138:chemical synthesis*; D004867:Equipment Design; D007553:Isotope Labeling / Q000295:instrumentation* / Q000379:methods*; D010880:Piperidines / Q000138:chemical synthesis*; D011312:Pressure; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
chemical_list: C443080:1-(1,4-benzodioxan-6-ylcarbonyl)piperidine; D002250:Carbon Radioisotopes; D004149:Dioxoles; D010880:Piperidines; D019275:Radiopharmaceuticals; D002248:Carbon Monoxide