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Specific tritium labelling of α ‐(p‐methoxyphenyl)‐α'‐nitro‐4 [3‐(dimethylamino) propoxy] stilbene (CI‐680) by catalytic deiodination
Author(s) -
Blackburn C. E.
Publication year - 1972
Publication title -
journal of labelled compounds
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0022-2135
DOI - 10.1002/jlcr.2590080212
Subject(s) - tritium , labelling , yield (engineering) , chemistry , nitro , catalysis , moiety , halogenation , tritium illumination , specific activity , medicinal chemistry , radiochemistry , nuclear chemistry , organic chemistry , materials science , alkyl , biochemistry , physics , nuclear physics , metallurgy , enzyme
In an unusual example of tritium‐labelling by catalytic dehalogenation in the presence of competing groups, an iodinated precursor was selectively deiodinated with tritium gas to yield α‐(4‐methoxyphenyl‐3‐ 3 H) ‐α'‐nitro‐4[3‐ (dimethylamino) propoxy] stilbene (CI‐680‐ 3 H). The product was labelled specifically at the C‐3 position of the methoxyphenyl moiety with a specific radioactivity of 27.7 Ci/mmole and a net yield of 609 mCi. Characterization of CI‐680‐ 3 H (base) established the chemical purity to be ≥99% and the radiochemical purity to be ≥97.6%. Characterization also included an evaluation of the tritium label stability in water and in aqueous acidic and basic media.