Imidazole derivatives having an inhibitory activity for farnesyl transferase and process for preparation thereof
申请人:LG Chemical Ltd.
公开号:US06268363B1
公开(公告)日:2001-07-31
The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.
base-catalyzed cascade nucleophilic/aza-Michael addition reaction of N-alkoxy β-oxo-acrylamides with isocyanates has been developed to afford various highly functionalized hydantoin derivatives in 80–98% yields under mild reaction conditions. The intriguing features of this method include metal-free reaction conditions, low catalyst loading, broad substrate scope and short reaction time.