发明名称 0,3-Diazacycloalkeno[2,1-a]isoindolones
摘要 1,191,240. 1,3 - Diazocycloalkeno[2,1-a]isoindolones. F. HOFFMANN-LA ROCHE & CO. A.G. 28 March, 1968 [18 May, 1967], No. 28273/69. Divided out of 1,191,237. Heading C2C. Novel compounds having the general formula I or II: wherein B represents an alkylene chain containing from 2 to 4 carbon atoms in which one or more of the hydrogen atoms may be replaced by lower alkyl having 1 to 6 carbon atoms and R<SP>1</SP> and R<SP>2</SP> individually represent a halogen atom or the trifluoromethyl or hydroxy group or a lower alkyl having 1 to 6 carbon atoms or lower alkoxy group having 1 to 6 carbon atoms and wherein the broken lines denote that the atoms or groups attached thereby are optional and the dots in the formulµ represent carbon atoms are prepared by (a) in the case of compounds having the Formula I heating the corresponding phthalaldehydic acid in ethanol with ethylenediamine (i.e. a diamine of the formula H 2 N-BNH 2 ) and addition of ethereal hydrogen chloride gives the hydrochloride salt; (b) in the case of compounds having the Formula II treating compounds of the Formula I with diethyll azodicarboxylate under reflux, removing the hydrazo ester by filtration and concentrating the filtrate to give the product of the Formula II. In the examples, 1,2,3,9b-tetrahydro-5H- imidazo[2,1-a]isoindolone- (5) hydrochloride, 1,2,3,9b - tetrahydro - 5H - imidazo[2,1-a]isoindolone-(5) and the corresponding 2,3-dihydro- 5H-imidazo[2,1-a]isoindolone-(5) are prepared.
申请公布号 GB1191240(A) 申请公布日期 1970.05.13
申请号 GB19690028273 申请日期 1968.03.28
申请人 F. HOFFMANN-LA ROCHE & CO., AKTIENGESELLSCHAFT 发明人
分类号 A61K31/00;C07C45/29;C07C45/41;C07C51/363;C07D209/44;C07D233/22;C07D487/04 主分类号 A61K31/00
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