| 摘要 |
N-alkyl or oxyalkyl arylpiperidine cpds. of formula (I) are new. In (I), Ar = Ph, fluorophenyl, chlorophenyl, trifluoromethylphenyl, methoxyphenyl, tolyl or naphthyl opt. substd. with F, Cl, CF3 or OMe; n= 2-4; X= O, S or a direct bond; R= Ph, hydroxyphenyl, methoxyphenyl, tolyl, 2-amino-4-thiazolylphenyl, 5-oxindolyl, 2-methyl-4-oxo-4H-pyrido (1,2a)pyrimidin-3-yl, 7,9-dioxo-8-azaspiro(4,5)decan-8-yl or 1,8,8-trimethyl-2,4-dioxo -3-azabicyclo(3.2.1)heptan-3-yl. - Also new are arylpiperidine cpds. (II) from which (I) are prepd.. - (I) can be prepd. by reacting (II) with at least an equiv. amt. in moles of an aralkyl (or aryloxyalkyl) or heterocyclyl ether deriv. or corresp. halide of formula: Q(CH2)nXR where Q= a leaving gp. (e.g. p-toluenesulphonyloxy or halogen) in a reaction-inert polar organic solvent (partic. acetone or MIBK), under anhydrous conditions, in the presence of at least an equiv. amt of an appropriate base (partic. Na2CO3 or K2CO3). A temp. of 50-150 deg.C for 2-24 hrs. is used. |
