PURPOSE: To provide a novel terfenadine derivative which exhibits high antihistaminic activities with fewer side effects and excellent persistency of effects and is useful for the treatment of allergic rhinitis, asthma, gastrointestinal ulcer and the like.
CONSTITUTION: There is provided a compound of formula I (wherein R1 is H or 1-6C alkyl, and is bonded to 1-or 2-position of a tetrazol ring; one of R2 and R3 is H and the other is OH) or a salt thereof, e.g. p-[1-hydroxy-4-(4- hydroxydiphenylmethyl-1-piperidinyl)butyl]-2-(1H-tetrazol-5-yl)-isopropylbenzene. The compound of formula I wherein R1 is H is obtained by reacting OH- protected 2-methyl-2-phenylpropanol with a γ-halogeno-butyryl halide to give a compound of formula II (wherein P is a protecting group; and Z is halogen), converting this into a compound of formula III, condensing the resultant with an azacyclonol to give a compound of formula IV and reacting this compound with an azide compound to form a tetrazole ring.
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