| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound having activity as an ORL1-receptor agonist, and useful for treating and preventing pain, inflammatory disease, etc. as the agonist. SOLUTION: This compound is shown by formula I [R1 and R2 are each H, a halogen, hydroxyl or the like; R3 and R4 are each H, a halo 1-10C alkyl, hydroxyl or the like; and R5 is H, a halogen, hydroxyl or the like] or its salt such as N-cyclohexyl-1-[1-(cyclooctylmethyl)-4-piperidinyl]-1H-benzimidazol-2- amine or its salt. The compound is obtained by subjecting a benzimidazolylpiperidine compound of formula II to reductive amination with an aldehyde compound of the formula R5-CHO, reacting the obtained compound with a proper nucleophilic reagent and introducing an eliminable group to the resultant substance in the presence or absence of a catalyst.
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