PURPOSE: To provide a new compound having acyl-CoA:cholesterol acyltrans ferase inhibitory activity, thus useful for the prevention and therapies of hypercholesterolemia, hyperlipemia and atherosclerosis.
CONSTITUTION: The objective compound of formula I (R1 is halogen, nitro, amino, aryl, etc.; R2 is H, alkyl, cycloalkyl, etc.; R3 is H, lower alkyl, aryl, etc.; R4 is H, halogen, lower alkyl, etc.; R5 is H, halogen, aryl, etc.; A is single bond or lower alkylene; X is O, S, NH, etc.), e.g. N-benzyl-N-[3-(4- chlorophenyl)-5-methylbenzofuran-2-ylmethyl]-N'-(2,4,6-trifluorophenyl)urea. The compound of the formula I can be obtained by reaction of a compound of formula R1-NCO with a compound of formula II in a solvent (e.g. methylene chloride) in the presence of a base (e.g. triethylamine) under cooling to room temperature.
ONE KAZUHIKO
TANAKA HIROKAZU
