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Mechanistic approach of the nucleophilic 18 F‐ exchange on 4′‐NO 2 ‐spiperone using TBA 18 F or K 2.2.2. /K 18 F
Author(s) -
Gysemans M.,
Mertens J.
Publication year - 1990
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.2580280109
Subject(s) - chemistry , butyrophenone , spiperone , yield (engineering) , stereochemistry , computational chemistry , radiochemistry , medicinal chemistry , thermodynamics , biochemistry , physics , receptor , neuroscience , dopamine , haloperidol , antagonist , biology
High yield single step preparation of 4′‐ 18 F‐spiperone by 18 F‐ for NO 2 exchange in highly basic conditions fails when using 4′‐NO 2 ‐spiperone as a precursor. This compound moreover inhibits radiofluorination of highly activated molecules in mentioned conditions. Inhibition is not provoced by ketalised analogues of the butyrophenone. This led to assume that enolisation of the butyrophenone was responsible for those phenomena. The assumption is supported by the fact that the results of inhibition experiments fit to a theoretical model.