C-11 radiochemistry in cancer imaging applications

Z. Tu, R. H. Mach

Research output: Contribution to journalArticlepeer-review

39 Scopus citations

Abstract

Carbon-11 (C-11) radiotracers are widely used for the early diagnosis of cancer, monitoring therapeutic response to cancer treatment, and pharmacokinetic investigations of anticancer drugs. PET imaging permits non-invasive monitoring of metabolic processes and molecular targets, while carbon-11 radiotracers allow a hot for cold supstitution of biologically active molecules. Advances in organic synthetic chemistry and radiochemistry as well as improved automated techniques for radiosynthesis have encouraged investigators in developing carbon-11 tracers for use in oncology imaging studies. The short half-life of carbon-11 (20.38 minutes) creates special challenges for the synthesis of C-11 labeled tracers; these include the challenges of synthesizing C-11 target compounds with high radiochemical yield, high radiochemical purity and high specific activity in a short time and on a very small scale. The optimization of conditions for making a carbon-11 tracer include the late introduction of the C-11 isotope, the rapid formation and purification of the target compound, and the use of automated systems to afford a high yield of the target compound in a short time. In this review paper, we first briefly introduce some basic principles of PET imaging of cancer; we then discuss principles of carbon-11 radiochemistry, focus on specific advances in radiochemistry, and describe the synthesis of C-11 radiopharmaceuticals developed for cancer imaging. The carbon-11 radiochemistry approaches described include the N,O, and S-alkylations of [11C]methyl iodide/[11C]methyl triflate and analogues of [11C]methyl iodide and their applications for making carbon-11 tracers; we then address recent advances in exploring a transmetallic complex mediated [11C]carbonyl reaction for oncologic targets.

Original languageEnglish
Pages (from-to)1060-1095
Number of pages36
JournalCurrent Topics in Medicinal Chemistry
Volume10
Issue number11
DOIs
StatePublished - 2010

Keywords

  • Cancer imaging
  • Carbon-11
  • Molecular imaging
  • Pet imaging
  • Radiochemistry
  • Radiosynthesis

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