Butyrophenone analogues in the carbazole series: Synthesis and determination of affinities at D-2 and 5-HT2a receptors

Authors
Masaguer, CE Formoso, E Ravina, E Tristan, H Loza, MI Rivas, E Fontenla, JA
Citation
Ce. Masaguer et al., Butyrophenone analogues in the carbazole series: Synthesis and determination of affinities at D-2 and 5-HT2a receptors, BIOORG MED, 8(24), 1998, pp. 3571-3576
Citations number
27
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
24
Year of publication
1998
Pages
3571 - 3576
Database
ISI
SICI code
0960-894X(199812)8:24<3571:BAITCS>2.0.ZU;2-T
Abstract
We describe a practical and efficient route for synthesis of 2-aminomethyl- 1,2,3,9-tetrahydro-4H-carbazol-4-ones using an effective Fisher indole meth odology. The most active compounds, 4b (QF 2003B) and 4c (QF 2003B), with p Ki (5-HT2A/D-2) ratio of 1.28 show an antipsychotic profile according to Me ltzer's classification, (C) 1998 Elsevier Science Ltd. All rights reserved.