Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors
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 discovery of the cis azetidinone 2c, which had improved CAI activity. Compound 2c was prepared using a selective reduction and silane mediated debromination to control the relative stereochemistry of the three centers.
McKittrick, BA; Ma, K; Dugar, S; Clader, JW; Davis, H; Czarniecki, M; McPhail, AT
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