Synthesis of no‐carrier‐added radiobrominated N‐alkylated analogues of spiperone

S. M. Moerlein, P. Laufer, G. Stöcklin

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The synthesis of a series of p‐bromo‐3‐N‐alkyl spiperone analogues is described. N‐alkylation was achieved via reaction of the potassium salt of the spiperone lactam ring with alkyl iodide; subsequent reactions with elemental bromine gave the p‐brominated isomers. Optimization studies using no‐carrier‐added (n.c.a.) 77Br indicated that radiobromination of N‐alkyl spiperone analogues occurs with higher yields and in shorter reaction times when dichloramine‐T (DCT) is used rather than H2O2/acetic acid as an oxidant. The production of the title compounds in high effective specific activity with radiochemical yields of 20–30 % using n.c.a. 77Br and DCT is reported.

Original languageEnglish
Pages (from-to)1007-1022
Number of pages16
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number10
StatePublished - Oct 1985


  • Br
  • Spiperone
  • brominated spiperone analogues
  • dopaminergic receptors
  • neuroleptic
  • no‐carrier‐added radiobromination


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