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

  作者 MOSELEY CHRISTIAN K; CARLIN STEPHEN M; NEELAMEGAM RAMESH; HOOKER JACOB M  
  选自 期刊  Organic Letters;  卷期  2012年14-23;  页码  5872-5875  
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[摘要]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.

 
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