A rapid method for the synthesis of 4-iodoantipyrine

Abstract

Summary: A modified method for the synthesis of radioiodinated 4-125iodoantipyrine based on electrophilic iodination using Na103 as an oxidising agent is described. This straightforward method is reproducible and yields consistently high ( > 9 8 % ) radiolabelled 4 ' 2 5~~P .The use of solid phase extraction columns facilitates the removal of excess iodide and chloride ions with consistently high recovery ( > 8 0 % ) , simplifies the purification procedure, reduces preparation time and does not require the use of hplc technique.

4-Iodoantipyrine synthesized by means of solid-state mechanical activation

“…1-Phenyl-2,3-dimethyl-4-iodopyrazolone (4-iodoantipyrine, I) is a well-known drug possessing anti-inflammatory, interferon-inducing, and virus-neutralizing properties, which is also used in the radioactively labeled form [1,2]. The wide use of this drug in the past decade is related to its unique effect in the prophylaxis and treatment of tick-borne encephalitis.…”