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Phosphinic acid analogues of γ‐aminobutyric acid (GABA). Synthesis of a new radioligand
Author(s) -
Hall Roger G.,
Kane Peter D.,
Bittiger Helmut,
Froestl Wolfgang
Publication year - 1995
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.2580360205
Subject(s) - chemistry , radioligand , aminobutyric acid , selectivity , stereochemistry , radioligand assay , receptor , combinatorial chemistry , biochemistry , catalysis
The synthesis of a new radioligand, which binds with high selectivity and affinity (K D = 7.4 nM) to the GABA‐B receptor, is described. A Wittig‐Horner approach was employed to prepare an unsaturated protected intermediate ( 6 ), suitable for tritiation and deprotection.