Abstract: A method for preparation of a cycloheptimidazole compound having formula (5),
wherein: R4 is a lower alkyl group, comprising reacting a compound of formula (1),
with an alkylamidine hydrochloride.
Abstract: The present invention relates to compounds of formula (1).
wherein: R1 is hydrogen atom or lower alkyl group, X is bromine atom or chlorine atom; and which are useful for the preparation of the cycloheptanoides such as cycloheptimidazole derivatives. The compound having formula (1) is obtained in a single pot by the reaction of a trialkylsilylether compound with a dihalocarbene which, in turn, is prepared from the reaction of chloroform or bromoform in the presence of base.
Abstract: New therapeutic agents of isoquinuclidine derivatives are represented by the following formula or its hydrochloride salts. ##STR1## (wherein R.sub.1 is hydrogen, carboxyl group, ethoxycarbonyl group, 4-(ethoxycarbonyl)phenyl group, 4-(carboxy)phenyl group, 2-(carboxy)-thiophene-5-yl group, quinoline-5-yl group, 4-(quinoline-5-yl)phenyl group or 4-(3-oxo-2-azabicyclo[2.2.2]octane-2-yl)-phenyl group; R.sub.2 is hydrogen or allyl group; Both X.sub.1 and X.sub.2 are hydrogen and X.sub.1 and X.sub.2 may form an oxo group; m stands for an integer of 0 to 2.) These compounds, have excellent inhibitory activities against squalene synthase, and are useful as a treatment agent for hypercholesterolemia.