To obtain a new compound useful as an anxiolytic containing a sedative component, having partial action on and antagonism against a 5-HT1A and antagonism against a H1 receptor.
This compound is shown by formula I (R is a monosubstituted or disubstituted phenyl, thienyl or adamanthyl which contains a substituent group such as fluoro or methoxy; R1 and R2 are each H, a halogen or methoxy) or its salt and/or its hydrate such as N-(2-[4-(2-fluoro-5-methoxyphenylmethyl) piperidin-1-yl]ethyl}-4-methoxybenzamide hydrochloride. The compound is preferably obtained by successively treating a piperidinyl intermediate of formula II with formula and potassium cyanide to give a nitrilopiperidine intermediate, catalytically reducing the intermediate, and acylating the prepared ethylamine intermediate with an acylating agent such as thionyl chloride. The compound of formula II is obtained, for example, from 4-cyanopyridine through a compound of formula III.
DANIERU JIEI KIIBUI
JIYON DEII KATSUTO
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