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Synthesis of tritium‐labelled 2‐(3′‐carboxypropyl)‐3‐imino‐6 para‐methoxy phenyl‐2,3‐dihydropyridazine ([ 3 H] SR95531)
Author(s) -
Gh A. Melikian,
Schlewer G.,
Hurt S.,
Chantreux D.,
Wermuth C. C.
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.2580240306
Subject(s) - chemistry , tritium , pyridazine , hydrolysis , alkylation , medicinal chemistry , stereochemistry , organic chemistry , catalysis , physics , nuclear physics
The synthesis of tritium labelled 2‐(3′‐carboxypropyl)‐3‐imino‐6‐para‐methoxyphenyl‐2,3‐dihydropyridazine, a new, specific, water‐soluble and chemically stable GABA antagonist at the GABA A receptor site is reported. The synthesis involves an N‐2 endo‐alkylation of 3‐amino‐6‐p‐methoxyphenyl‐pyridazine with ethyl γ‐bromocrotonate, reductive tritiation of the crotonic double bond and hydrolysis in acidic medium.