To obtain new derivative of piperidine having blocking affect to muscarine receptor useful for therapy of neurogenic bladder, unstable bladder, irritable intestine syndrome or the like.
The compound is expressed by formula I [n is an integer of 1 to 5; R is H; R1 is (methylenedioxy)phenyl or (ethylenedioxy)phenyl or 2,3- dihydrobenzofuranyl or the like; R2 is phenyl or a 3 to 6C cycloalkyl; R3 is H or OH or the like; W is O or S]. For example, 4-(diphenylhydroxymethyl)-1-{3-[3,4-(ethylenedioxy)phenoxy]propyl}-piperidine. The compound of formula I is obtained by reacting the compound of the formula R1-WH and the compound of the formula X-(CH2)n-OH (X is Cl or Br or the like) in the presence of a base to obtain the compound of the formula R1- W-(CH2)n-OH, reacting this compound with a halogenating agent or the like such as thionyl chloride to obtain R1-W-(CH2)n-Y (Y is Cl or Br or the like), subsequently reacting the compound of formula II to this compound.
KONDO KAZUYUKI
OTA TOMOKI
TOMIZAWA KAZUYUKI