| 摘要 |
<p>Oxazolidinones of formula (I) are new. (R1 is 4-NH2, 2-NMe2, 4-(n-pentylamino), 4-CF3, 4-phenoxymethyl (opt. ring substd. by 3-NO2), 4-(2-chlorophenylethyl), trans-4-styryl or 4-(2-2-methylthio-1,3-dioxolan) gp.; R1 may also be 4-SR1, 4-OR2 4-benzyloxy ring substd. by R3 or by R4 and R5, 4- HetCH2O, 4-COR6, 2- or 4- OCH2COR7, 2- or 4- O(CH2)nCN or at 4-posn. methoxymethoxy, 2-morpholinoethoxy or the oxime of acetylmethoxy; R1 is 5C alkyl or acetylmethylthio; Ri is iso- or neo-pentyl, 3,3-dimethylbutyl, 2-ethylbutyl, cycloalkyl (3-7C) methyl, cycloalkyl(5-6C)ethyl, penten-4-yl, 6-7C cycloalken-1-yl-methyl, 1-methylcyclopentylmethyl or cyclohexadien-1,4-ylmethyl, 1,3-dioxolan-2-ylmethyl (and corresp. rings with 1 or both O replaced by S), 1,3-dithian-2-ylmethyl or tetrahydropyran -2,3 or 4-ylmethyl; R3 is 3-CN, 2-Cl, 2-2-Br, 2-I,2-NO2, 2-CN, 4-CH3CONH, 2-NH2, 4-NHCOOCH3 or 4-NHCOC2H5; R4 and R5 are 3,4-Cl2, 2,4-Cl2, 3,5-Cl2, 3-Cl-4-F, 3-NO2-4-F, 3-NO2-5-CN. 3-NO2-5-Cl.3-NO2-4-Cl, 3-Cl-4-NO2 or 3-CN-4-F; Het is 2,3 or 4-pyridyl, 2-or 3-thienyl, 2- or 3-furyl or 2-&yrazinylf R6 is 2-3C alkyl; R7 is 1-3C alkyl; and n is 1-4). (I) have antidepressant activity at least equal to toloxatone. A typical cpd. is 3-(4- 2-cyanoethoxy phenyl)-5-hydroxymethyl-2-oxazolidinone.</p> |
