Radiopharmaceuticals. 12. New Rapid Synthesis of Carbon-11 Labeled Norepinephrine Hydrochloride

Joanna S. Fowler, Robert R. MacGregor, Azizullah N. Ansari, Harold L. Atkins, Alfred P. Wolf

Research output: Contribution to journalArticlepeer-review

36 Scopus citations

Abstract

The rapid growth in the use of radiopharmaceuticals for external radioscanning has resulted in an increasing need for new safer radiopharmaceuticals labeled with elements emitting radiation which can be detected outside the body barrier. The potential impact of organ-specific radiopharmaceuticals labeled with short-lived nuclides on the safety of diagnostic procedures has justified expending considerable effort in the development of rapid organic synthetic procedures in order to accomplish the incorporation of simple labeled precursors into relatively complex molecules of pharmacological interest.1,2 One of the more potentially useful radionuclides for labeling is 11C which decays by positron emission and has a half-life of 20.4 min. The advantage of 11C for diagnostic procedures lies in its short half-life (which lowers the radiation dose to the patient) and positron emission (which offers improved resolution on scanning by detection of the 511-keV annihilation radiation). In addition, since carbon is naturally occurring the properties of the normal bioactive molecules are not significantly altered by labeling. However, the reduced time scale in which one must work, as well as the limited number of readily available nC-labeled precursor molecules1 (for example 11CO, 11CO2, 11CH2O, H11CN, H11C = 11CH, etc.), presents certain restrictions on the nature of the 11C-labeled radiopharmaceuticals which one can prepare employing syntheses described in the chemical literature.

Original languageEnglish
Pages (from-to)246-248
Number of pages3
JournalJournal of Medicinal Chemistry
Volume17
Issue number2
DOIs
StatePublished - 1 Feb 1974
Externally publishedYes

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