PURPOSE: To obtain new 4-aminomethylpiperidine derivatives useful for the treatment of anxiety, depression, and somnipathy, etc.
CONSTITUTION: This compd. is a deriv. of the formula I [wherein each of A and B is O, S or methylene; (n) is 0 or 1; R1 is H or 1-4C alkyl; Y is carbonyl or methylene; Ar is (halogen- or 1-4C alkyl-substd.) phenyl], as well as its pharmacological acceptable salts with inorg. acid or org. acid, such as 1-(3-methyl- benzoyl)-4-(indan-2-yl-methylaminomethyl)piperidine. An amine of the formula II is allowed to react with a compd. of the formula III (wherein X is a distal group from nucleus such as methylsulfonyloxy and benzenesulfonyloxy) in a solvent such as toluene and xylene preferably at 50-160°C optionally in the presence of an org. base such as tertiary amine.
DOUNI BIGU