An Efficient and Practical Radiosynthesis of [C-11]Temozolomide

作者：Moseley Christian K; Carlin Stephen M; Neelamegam Ramesh; Hooker Jacob M^*

来源：Organic Letters, 2012, 14(23): 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, [C-11]TMZ, has been utilized to help elucidate the mechanism and biodistribution of TMZ. Challenges in [C-11]TMZ synthesis and reformulation make it difficult for routine production. A highly reproducible one-pot radiosynthesis of [C-11]TMZ with a radiochemical yield of 17 +/- 5% and >= 97% radiochemical purity is reported.

• 出版日期2012-12-7