Synthesis of "no-carrier-added" carbon-11 SarCNU: the sarcosinamide analog of the chemotherapeutic agent BCNU.
Carbon-11-labeled SarCNU [N-(2-chloroethyl)-N-nitroso-N'-(carboxamidomethylene)-N'-(methyl) - [11C]-urea], a potential chemotherapeutic agent, has been prepared by the nitrosation of the corresponding urea, N-(2-chloroethyl)-N'-(carboxamidomethylene)-N'-(methyl) [11C]urea (SarCU). SarCU was prepared by reacting sarcosinamide with [11C]-2-chloroethylisocyanate, which was itself prepared by reacting [11C]-phosgene with 2-chloroethylamine hydrochloride suspended in dioxane. The synthesis yielded [11C]SarCNU with an average radiochemical purity of 95% in an average overall radiochemical yield of 18% relative to the activity measured at the end of [11C]phosgene introduction.
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McConnell Brain Imaging Centre, Montreal Neurological Institute and Hospital, Canada.
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D000970:Antineoplastic Agents / Q000138:chemical synthesis; D002250:Carbon Radioisotopes; D002330:Carmustine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D007553:Isotope Labeling; D008722:Methods
D000970:Antineoplastic Agents; D002250:Carbon Radioisotopes; C044565:2-((((2-chloroethyl)nitrosoamino)carbonyl)amino)propanamide; D002330:Carmustine