| 摘要 |
PURPOSE:To obtain the titled compound useful as a nuclear medicine diagnosticum of dopamine acceptor and radioactive drugs in high yields, by reacting a 2-bromobutyrophenone derivative with a radioactive metallic iodide in a polar solvent in the presence of a copper salt and a sulfonic acid. CONSTITUTION:A 2-bromobutyrophenone derivative (e.g. 2-bromospiroperidol, etc.) shown by formula I [R is group shown by formula II, formula III or formula IV (R1 is H or lower alkyl; R2 is H, halogen, lower alkyl, lower haloalkyl or lower alkoxy; R3 is H, lower alkyl and dotted line is single bond or double bond)] and a radioactive metallic iodide [e.g. Na<125>I, etc.] are subjected to exchange reaction in a polar solvent such as acetonitrile, etc., in the presence of both a copper salt (e.g. copper sulfate, etc.) and a sulfonic acid (e.g. naphthalenesulfonic acid, etc.) at about 50-180 deg.C to give a radioactive a 2- bromobutyrophenone derivative [e.g. [<125>I]-2-iodospiroperidol, etc.] shown by formula V (I* is radioactive iodine atom).
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