Synthesis of 123I‐labelled 4‐iodo‐2, 5‐dimethoxyphenylisopropylamine
Gisela Braun, Alexander T. Shulgin, Thornton W. Sargent
Journal of Labelled Compounds and Radiopharmaceuticals 1978 DOI: 10.1002/jlcr.2580140515 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Method development Peer reviewed |
|---|---|
| Keywords | Radiochemistry Radiosynthesis Radioactive labeling Isotope tagging Iodine-123 labeling Tracer synthesis Radiopharmaceutical production Brain chemistry Brain research Neurobiology Psychopharmacology Brain function Mental health research Drug tracking Psychotomimetic agents Substance research Drug action Pharmaceutical research Drug development Molecular imaging In vivo tracking Diagnostic tracers Biomedical imaging Brain imaging Spect imaging |
| Citations | 9 |
| Key points | A rapid synthesis of 4-iodo-2,5-dimethoxyphenylisopropylamine with 123I was achieved in less than one half-life with 10% overall yield. |
Abstract
AbstractA rapid and convenient synthesis of the psychotomimetic agent 4‐iodo‐2, 5‐dimethoxyphenylisopropylamine is described, incorporating the radioisotope 123I (T1/2 13 hr). With the amine function of 2, 5‐dimethoxyphenylisopropylamine blocked as the phthalimide, it was found that the aromatic 4‐position could be directly iodinated with iodine monochloride. The phthalic acid moiety was rapidly removed with hydrazine in butanol to provide the title compound, as the hydrochloride salt, in an overall yield of 10% and in a reaction time of less than one half‐life.