PURPOSE: To obtain a new quinuclidine derivative suppressing the biosynthesis of cholesterol by inhibiting squalene formation.
CONSTITUTION: This derivative (salt) is shown by formula I [R1 is a (substituted) phenyl or a (substituted) pyridyl; R2 is a 5-9C alkylene, a 5-9C alkenylene or a 5-9C alkynylene; R3 to R5 are: (R3, R4, R5)=(O, H, H), (O-CH2, H, H) or R4 and R5 are bonded to form a double bond] such as 3-{5-[4-(3-methylphenoxy) phenyl]-2-pentenyloxy}-1-azabicyclo[2,2,2]octane. The derivative, for example, is obtained by reacting a compound of the formula R1-R2-X (X is a halogen, an alkylsulfonic acid ester, etc.) with a compound of formula II in an inert solvent in the presence of a base at 0-100°C (preferably 0-25°C) for 1-48 hours (preferably 12-24 hours) to give a compound of formula III and removing the amino-protecting group, borane.
ISHIKAWA AKIRA
TAMURA KUNIO
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