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    • 10. 发明授权
    • 3-Aryl 2-oxazolidinones, their process of preparation and their
therapeutical application
    • 3-芳基2-恶唑烷酮,其制备方法及其治疗应用
    • US4150029A
    • 1979-04-17
    • US771814
    • 1977-02-23
    • Philippe L. DostertColette A. DouzonGuy R. BourgeryClaude J. GouretGisele C. MocquetJean A. Coston
    • Philippe L. DostertColette A. DouzonGuy R. BourgeryClaude J. GouretGisele C. MocquetJean A. Coston
    • A61K31/42A61K31/421A61P25/24A61P25/26C07D263/24
    • C07D263/24
    • Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or CONHR.sub.7 and R.sub.7 is methyl or isopropyl,And whereinWhen R.sub.1 is hydrogen: R is p-nitro, p-cyano; p-aldehydo; p-acetyl; m-ethyl; m-nitro; m-bromo; 3,4-dimethyl; m-NH.sub.2 ; p-methylamino; p-dimethylamino; p-diethylamino; p-methylbenzylamino; p-pyrrolidino; p-piperidino; SR.sub.4 in para position in which R.sub.4 is alkyl having 1 to 4 carbon atoms or cyclohexyl; OR.sub.5 is para position in which R.sub.5 is alkyl having 2 to 7 carbon atoms, cyclohexyl, cyclohexylmethyl, acetylmethyl; cyanomethyl, alkene-2 yl having 3 to 5 carbon atoms, butene-3 yl, cyclohexene-1 methyl, propargyl, butyne-2 yl, ##STR2## in which n is one or 2 and when n is one, R.sub.6 is hydrogen, o-fluoro, o-methyl, m-chloro, m-fluoro, m-methyl, m-trifluoromethyl, p-chloro, p-bromo-, p-fluoro, p-cyano, p-nitro or p-dimethylamino and when n is 2, R.sub.6 is hydrogen; and 3-methyl-4-benzyloxy:When R.sub.1 is CONHR.sub.7 and R.sub.7 is methyl: R is m-trifluoromethyl; m-bromo; p-chloro; p-fluoro; 3,4-dichloro; p-thiomethyl; p-acetyl; OR.sub.8 in para position wherein R.sub.8 is alkyl having 2 to 5 carbon atoms, cyanomethyl, acetylmethyl, propargyl or ##STR3## in which R.sub.9 is hydrogen, m-chloro, m-bromo, m-fluoro, p-fluoro, p-chloro or p-nitro;And when R.sub.1 is CONHR.sub.7 and R.sub.7 is isopropyl; R is m-trifluoromethyl or p-benzyloxy.The compounds are prepared by cyclizing 1-phenylamino-2,3-propandiol derivatives to form 5-hydroxymethyl-3 phenyl-2-oxozolidinone derivatives. The 5-hydroxymethyl group can be transformed to --CH.sub.2 OCONHR.sub.7 by reaction with methyl isocyanate or isopropyl isocyanate. The compounds possess psychotropic, particularly antidepressant, activity.
    • 具有式“IMAGE”的化合物,其中R1是氢或CONHR7,R7是甲基或异丙基,当R1是氢时,R是对硝基,对氰基; 对醛 对乙酰基; 甲基; 间硝基 溴代 3,4-二甲基 m-NH2; 对甲基氨基; 对二甲基氨基; 对二乙基氨基; 对甲基苄基氨基; 对 - 吡咯烷子; 对哌啶子 其中R4是具有1-4个碳原子的烷基的对位的SR4或环己基; OR5是R5是具有2至7个碳原子的烷基的对位,环己基,环己基甲基,乙酰基甲基; 氰基甲基,具有3至5个碳原子的烯-2,丁烯-3,环己烯-1甲基,炔丙基,丁炔-2基,其中n为1或2,当n为1时,R6为氢, 邻 - 甲基,间 - 氯,间氟,间甲基,间三氟甲基,对氯,对溴 - ,对氟,对氰基,对硝基或对二甲基氨基,当 n为2,R6为氢; 和3-甲基-4-苄氧基: