New features in synthesis of talampanel related 2,3-benzodiazepines.
Analogues of talampanel (1), a highly active AMPA antagonist 2,3-benzodiazepine, were synthesized, where the characteristic amino-function was either transposed or sterically shielded. For the key intermediates (hemiketals 6a, b) a new synthetic method of different mechanism was developed. The inactivity of several new compounds indicates the significance of the 4-amino(phenyl) function in BDZs of type 1.
Sólyom
Sándor
S
IVAX Drug Research Institute Ltd., H-1045 Budapest, Berlini u. 47-49, Hungary. sandor.solyom@idri.hu
Pallagi
István
I
Abrahám
Gizella
G
Kertész
Máriusz
M
Horváth
Gyula
G
Berzsenyi
Pál
P
D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry; D008968:Molecular Conformation; D013237:Stereoisomerism
D001569:Benzodiazepines; C085266:talampanel