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75,77 Br‐Nor‐zimelidine: Radiohalogenation of a complex molecule via a trimethylstannyl precursor
Author(s) -
Kloster Gerd,
Laufer Peter,
Hanuš Jan
Publication year - 1985
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580220412
Subject(s) - chemistry , yield (engineering) , high performance liquid chromatography , molecule , medicinal chemistry , chromatography , organic chemistry , nuclear chemistry , combinatorial chemistry , materials science , metallurgy
Abstract 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 (II). (II) was prepared from NaSn (CH 3 ) 3 and nor‐zimelidine in low yield and thoroughly purified by preparative hplc. Bromodemetallation reaction using an equimolar amount of Br 2 showed quantitative formation of nor‐zimelidine without any detectable side‐products. Radiobromination yields using n.c.a. 75,77 Br at the 100 μCi level were 60 % with one hour preparation time including purification. Conditions were not optimized for large scale production of high specific activity (III) since the compound was withdrawn from the market by the producer during the course of this study.