PET studies of potential chemotherapeutic agents--X. Synthesis of "no-carrier-added" (11C)-HECNU: the hydroxyethyl analog of the chemotherapeutic agent BCNU.
Carbon-11-labeled HECNU [1-(2-chloroethyl)-1-nitroso-3-(2-hydroxyethyl) urea] a potential chemotherapeutic agent, has been prepared by the nitrosation of the corresponding carbon-11-labeled urea, HECU, [1-(2-chloroethyl)-3-(2-hydroxyethyl) urea]. The isometric byproduct of nitrosation, 1-(2-chloroethyl)-3-nitroso-3-(2-hydroxyethyl) urea can be efficiently removed by preparative scale HPLC on a Partisil column. (11C)-HECU was prepared by reacting ethanolamine with (11C)-2-chloroethyl-isocyanate which was itself prepared by reacting [11C)-phosgene with 2-chloroethylamine hydrochloride suspended in dioxane at 60-65 degrees C. This synthesis yielded (11C)-HECNU with an average radiochemical purity of 98% in an average radiochemical yield of 18% relative to the radioactivity measured at the end of the 11C-phosgene introduction.
Conway
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McConnell Brain Imaging Centre, Montreal Neurological Institute and Hospital, Quebec, Canada.
Diksic
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D002250:Carbon Radioisotopes; D007553:Isotope Labeling; D009607:Nitrosourea Compounds / Q000138:chemical synthesis*; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D009607:Nitrosourea Compounds; C013876:elmustine