Moseley, Christian K., Stephen M. Carlin, Ramesh Neelamegam, and Jacob M. Hooker. 2012. “An Efficient and Practical Radiosynthesis of [11C]Temozolomide.” Organic Letters 14 (23) (December 7): 5872–5875. doi:10.1021/ol302791x.
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.