| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new benzimidazole derivative having a oxidized functional group in the phenyl substitution group showing H1 -antihistaminic activities without cardiotoxicity and useful as a treating agent, etc., for an allergic state. SOLUTION: This new benzimidazole derivative is the one represented by formula I [R1 is H, methyl, ethyl, isopropyl, cyclopropyl or vinyl; R2 is CH2 OH, COOH, COOR3 (R3 is the R1 ), 4,4-dimethyl-2-oxazolinyl] or its salt of a pharmaceutically permissible acid or base, e.g. 1-(2-ethoxyethyl)-2-[1-[2-[4-[1-(4,4- dimethyl-Δ<2> -oxazolin-2-yl)-1-methylethy]phenyl]ethyl]piperidin-4-yl]-1H benzimidazole. The compound of formula I in which e.g. R1 is an alkyl and R2 is 4,4-dimethyl-2-oxozolinyl is obtained by reacting a compound of formula II with a compound of formula III to provide a compound of formula IV and further N-alkylating the compound of formula IV again.
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