Synthesis of tritiated clenbuterol

Ilan Pri‐Bar, Ouri Buchman

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

Tritiated clenbuterol was prepared starting from 4‐aminoacetophenone (I) which was selectively brominated to 4‐amino‐3,5‐dibromoacetopheno ne (II), then to 4‐amino‐α,3,5‐tribromoacetophenone (III) and reacted with tert.butylamine to 4‐amino‐3,5‐dibromo‐α‐tert.butylaminoacetoph‐none(IV). (IV) was dehalogenated and reduced with tritium gas to give 2‐(tert.butylamino)‐1‐(4‐amino‐[3,5‐3H]‐phenyl)‐[1‐3H]‐ethanol (V). This tritiated compound underwent selective aromatic chlorination to give the desired 2‐(tert.butylamino)‐1‐(4‐amino‐3,5‐dichlorophenyl)‐[1‐3H]‐ethanol, [ethanol‐1‐3H]clenbuterol, with specific activity of 13.4 Ci/mmol (496 GBq/mmol).

Original languageEnglish
Pages (from-to)1393-1400
Number of pages8
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume28
Issue number12
DOIs
StatePublished - 1 Jan 1990
Externally publishedYes

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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