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An Efficient and Practical Radiosynthesis of [11C]Temozolomide

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journal contribution
posted on 07.12.2012, 00:00 by Christian K. Moseley, Stephen M. Carlin, Ramesh Neelamegam, Jacob M. Hooker
Temozolomide (TMZ) is a prodrug for an alkylating agent used for the treatment of malignant brain tumors. A positron emitting version, [11C]TMZ, has been utilized to help elucidate the mechanism and biodistribution of TMZ. Challenges in [11C]TMZ synthesis and reformulation make it difficult for routine production. A highly reproducible one-pot radiosynthesis of [11C]TMZ with a radiochemical yield of 17 ± 5% and ≥97% radiochemical purity is reported.