Synthesis of 75Se-2-phenyl-1,2-benzisoselenazol-3(2H)-one (PZ 51; ebselen. A novel biologically active organo-selenium compound

✍ Scribed by R. Cantineau; G. Tihange; A. Plenevaux; L. Christiaens; M. Guillaume; A. Welter; N. Dereu

• Publisher: John Wiley and Sons
• Year: 1986
• Tongue: French
• Weight: 256 KB
• Volume: 23
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580230108

✦ Synopsis

The preparation o f 75Se-ebselen (75Se-PZ 51) i n a high radiochemical y i e l d (%40 %) and w i t h a s p e c i f i c a c t i v i t y o f 240 mCi/mM (8.9 GBq/mM) i s described. I t e n t a i l s a very simple, f a s t and one-pot procedure s t a r t i n g from elemental 75~e-seleni urn. 75Se-diselenosalicylic a c i d 4 i s i n i t i a l l y prepared as the key intermediate which i s trZnsformed i n t o a corresponding dichloride 5-before reacting w i t h a n i l i n e t o y i e l d the des i r e d 75Se-aselen. I d e n t i t y and p u r i t y o f the labelled compound were controll e d by comparison i n TLC, HPLC and MS w i t h an authentic sample (1-2).