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New Features in Synthesis of Talampanel Related 2,3-Benzodiazepines

[ Vol. 1 , Issue. 5 ]

Author(s):

S. Solyom, I. Pallagi, G. Abraham, M. Kertesz, G. Horvath and P. Berzsenyi   Pages 481 - 485 ( 5 )

Abstract:


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.

Keywords:

oxidation, isochromane, hemiketal, benzodiazepine, metabolism

Affiliation:

IVAX Drug Research Institute Ltd., H-1045 Budapest, Berlini u. 47-49, Hungary.



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