An efficient and practical radiosynthesis of [11C]temozolomide

Christian K. Moseley; Stephen M. Carlin; Ramesh Neelamegam; Jacob M. Hooker

doi:10.1021/ol302791x

An efficient and practical radiosynthesis of [¹¹C]temozolomide

Christian K. Moseley, Stephen M. Carlin, Ramesh Neelamegam, Jacob M. Hooker

Research output: Contribution to journal › Article › peer-review

13 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	5872-5875
Number of pages	4
Journal	Organic Letters
Volume	14
Issue number	23
DOIs	https://doi.org/10.1021/ol302791x
State	Published - Dec 7 2012
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry

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10.1021/ol302791x

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AU - Moseley, Christian K.

AU - Carlin, Stephen M.

AU - Neelamegam, Ramesh

AU - Hooker, Jacob M.

PY - 2012/12/7

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AB - 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.

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JF - Organic Letters

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