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An efficient and practical radiosynthesis of [11C]temozolomide.


ABSTRACT: Temozolomide (TMZ) is a prodrug for an alkylating agent used for the treatment of malignant brain tumors. A positron emitting version, [(11)C]TMZ, has been utilized to help elucidate the mechanism and biodistribution of TMZ. Challenges in [(11)C]TMZ synthesis and reformulation make it difficult for routine production. A highly reproducible one-pot radiosynthesis of [(11)C]TMZ with a radiochemical yield of 17 ± 5% and ?97% radiochemical purity is reported.

SUBMITTER: Moseley CK 

PROVIDER: S-EPMC3979304 | biostudies-literature | 2012 Dec

REPOSITORIES: biostudies-literature

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An efficient and practical radiosynthesis of [11C]temozolomide.

Moseley Christian K CK   Carlin Stephen M SM   Neelamegam Ramesh R   Hooker Jacob M JM  

Organic letters 20121114 23


Temozolomide (TMZ) is a prodrug for an alkylating agent used for the treatment of malignant brain tumors. A positron emitting version, [(11)C]TMZ, has been utilized to help elucidate the mechanism and biodistribution of TMZ. Challenges in [(11)C]TMZ synthesis and reformulation make it difficult for routine production. A highly reproducible one-pot radiosynthesis of [(11)C]TMZ with a radiochemical yield of 17 ± 5% and ≥97% radiochemical purity is reported. ...[more]

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