STEREOSELECTIVE SYNTHESIS AND BIOLOGICAL-ACTIVITY OF CIS AZETIDINONESAS CHOLESTEROL ABSORPTION INHIBITORS

Authors
MCKITTRICK BA MA K DUGAR S CLADER JW DAVIS H CZARNIECKI M MCPHAIL AT
Citation
Ba. Mckittrick et al., STEREOSELECTIVE SYNTHESIS AND BIOLOGICAL-ACTIVITY OF CIS AZETIDINONESAS CHOLESTEROL ABSORPTION INHIBITORS, Bioorganic & medicinal chemistry letters, 6(16), 1996, pp. 1947-1950
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
16
Year of publication
1996
Pages
1947 - 1950
Database
ISI
SICI code
0960-894X(1996)6:16<1947:SSABOC>2.0.ZU;2-S
Abstract
The C-3 sidechain of azetidinones related to SCH 48461 was modified by introducing a hydroxyl group at the 1' position. This led to the disc overy of the cis azetidinone 2c, which had improved CAI activity. Comp ound 2c was prepared using a selective reduction and silane mediated d ebromination to control the relative stereochemistry of the three cent ers. Copyright (C) 1996 Elsevier Science Ltd