75,77Br-Nor-zimelidine: Radiohalogenation of a complex molecule via a trimethylstannyl precursor
✍ Scribed by Gerd Kloster; Peter Laufer; Jan Hanuš
- Book ID
- 102372575
- Publisher
- John Wiley and Sons
- Year
- 1985
- Tongue
- French
- Weight
- 265 KB
- Volume
- 22
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
This communication describes the preparation of radiobrominated nor-zimelidine (III), a potential tracer for the serotonin reuptake system of the brain, by a bromodemetallation reaction using a suitable trimethylstannyl precursor ( 11). ( 11) was prepared from NaSn(CH3)3 and nor-zimelidine in low yield and thoroughly purified by preparative hplc. Bromodemetallation reaction using an equimolar amount of Br2 showed quantitative formation of nor-zimelidine without any detectable side-products. Radiobromination yields using n.c.a. 75r77Br at the loo pCi level were 60 % with one hour preparation time including purification.Conditions were not optimized for large scale production of high specific activity (111) since the compound was withdrawn from the market by the producer during the course of this study.