Perhydro-1,3-diazepine-2,4-diones by cyclization of 4-ureidobutyric acids with thionyl chloride: A reinvestigation
The structures of the previously reported aryl-perhydro-1,3-diazepine- 2,4-diones are shown to be pyrrolidinone carboxamide derivatives by nmr spectroscopy.
Heckendorn, Roland,Winkler, Tammo
p. 111 - 114
(2007/10/03)
Pharmacological evaluation of new baclofen derivatives
The synthesis and in-vivo central pharmacological properties, in particular antinociceptive activity, of some new baclofen derivatives is described. The delayed antinociceptive activity of the N-trifluoroacetyl analogue of baclofen is also characterized.
Synthesis of new 6-(4-chlorophenyl)perhydro-1,3-diazepine-2,4-diones via ureidobutyric acids
Synthesis of new 6-(4-chlorophenyl)perhydro-1,3-diazepine-2,4-diones was accomplished starting from 4-amino-3-(4-chlorophenyl)butyric acid (Baclofen). The chemical pathway involved the cyclisation of various 3-(4-chlorophenyl)- 4-ureidobutyric acids. However, none of the new derivatives retained the anticonvulsant activity of their six-membered ring homologues, belonging to the phenylpyrimidinedione series which we recently described.