A CHEMICAL METHOD FOR THE PREPARATION OF NOVEL 1,5-BENZODIAZEPINES ACTING AS CCK-B ANTAGONISTS IN HIGH ENANTIOMERIC PURITY

Authors
CUROTTO G DONATI D FINIZIA G URSINI A
Citation
G. Curotto et al., A CHEMICAL METHOD FOR THE PREPARATION OF NOVEL 1,5-BENZODIAZEPINES ACTING AS CCK-B ANTAGONISTS IN HIGH ENANTIOMERIC PURITY, Tetrahedron, 53(21), 1997, pp. 7347-7364
Citations number
32
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron → ACNP
ISSN journal
00404020
Volume
53
Issue
21
Year of publication
1997
Pages
7347 - 7364
Database
ISI
SICI code
0040-4020(1997)53:21<7347:ACMFTP>2.0.ZU;2-X
Abstract
A series of new N-(1,5-benzodiazepin-3-yl)-N'-arylureas, 2, bearing an alkyl substituent at the N5 position of the benzodiazepine nucleus ha s been studied as potential CCK-B antagonists. The homochiral compound s were obtained by resolving their precursors (amines 4) with a new re solution method based on the reaction between the amines and the chira l auxiliary 5, the subsequent separation of the diastereomers (6 and 7 ) and the eventual removal of the auxiliary moiety by hydrogenation. T he resolved amines and the corresponding final ureas showed good enant iomeric excesses. (C) 1997 Elsevier Science Ltd.