An Efficient and Practical Radiosynthesis of [11C]Temozolomide

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• 作者：Christian K. Moseley ; Stephen M. Carlin ; Ramesh Neelamegam ; Jacob M. Hooker
• 刊名：Organic Letters
• 出版年：2012
• 出版时间：December 7, 2012
• 年：2012
• 卷：14
• 期：23
• 页码：5872-5875
• 全文大小：256K
• 年卷期：v.14,no.23(December 7, 2012)
• ISSN：1523-7052

文摘

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 卤 5% and 鈮?7% radiochemical purity is reported.