| 摘要 |
<p>Oxazolidine derivs. of formula (I) are new. (R1 = H or CONHR7,R7 = CH3 or isopropyl., when R1 = H R may be p-NO2, p-NO2, p-CN, p-HCO, p-acetyl, methyl, m-NO2, m-Br, m-p dimethyl, m-NH2, p-NR2R3, p-SR4 or p- OR5. R2 and R3 are (H,CH3), (CH3, CH3), (C2H5, C2H5), (CH3, benzyl) or together complete pyrrolidino or piperidino. R4 = 1-4C alkyl or cyclohexyl. R5 = 2-7C alkyl, cyclohexyl, cyclohexylmethyl, acetylmethyl, cyanomethyl, 3-5C alken-2-yl, buten-3-yl-, cyclohexen-1-methyl, propargyl, butyn-2-yl or:- n = 1 and R6 = H,F (any position), CH3 (o or m), Cl (m or p) m-CF3, p-Br, p-CN, p-NO2 or p-(CH3)2N; or n = 2 and R6 = H or R is m-CH3 plus p-benzyloxy. When R7 = CH3, R may be m-CF3, m-Br, p-Cl, p-F, m-p-dichloro, p-CH3S, p-acetyl or OR8. R8 = 2-5C alkyl, cyanomethyl, acetylmethyl, propargyl, or R9 - substd. benzyl R9 = H, m or p-Cl, m or p.F, m - Br, p-NO2. When R7 =isopropyl, R is m-CF3 or p-benzyloxy). (I) have psychotropic activity and are useful as antidepressants. The LD50 for 6 cpds. quoted (orally in mice) is >1 g/kg 1.05 g/kg and for 4, >2g/kg.</p> |
