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No‐carrier‐added radiobromination via the gattermann reaction. — Synthesis of 75Br‐ and 77Br‐bromperidol —
Author(s) -
Suehiro Makiko,
Yokoi Fuji,
Nozaki Tadashi,
Iwamoto Masako
Publication year - 1987
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.2580241002
Subject(s) - chemistry , bromine , yield (engineering) , chlorine , copper , neutron activation analysis , halogen , catalysis , nuclide , regioselectivity , neutron activation , radiochemistry , organic chemistry , nuclear chemistry , neutron , physics , quantum mechanics , materials science , alkyl , metallurgy
The Gattermann reaction was applied to the no‐carrier‐added radiobromination of bromperidol. The synthesis with diazotized precursor, no‐carrier‐added 75Br‐ or 77Br‐, and copper powder proved to give the radiobrominated neuroleptic drug in high radiochemical yield of 60 ‐ 70%, and in high specific activity (∼5 Ci/umole). The radiobromination also proved to be regioselective. In the reaction, the copper catalyst was observed to play an important role. Formation of unlabeled by‐products due to stable chlorine or bromine contamination in the reaction mixture was also studied by neutron activation analysis. Removal of such undesirable halogen nuclides and separation of the unavoidably‐formed chlorinated coupound from the radiobrominated bromperidol is discussed.