首页> 外国专利> 6-X-(2-HYDROXYETHYL)AMINOALKYL-5,11-DIOXO-5,6-DIHYDRO- 11H-INDENO 1,2-CISOQUINOLINES OR SALTS THEREOF WITH INORGANIC AND ORGANIC ACIDS, METHODS OF PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION BASED THEREON

6-X-(2-HYDROXYETHYL)AMINOALKYL-5,11-DIOXO-5,6-DIHYDRO- 11H-INDENO 1,2-CISOQUINOLINES OR SALTS THEREOF WITH INORGANIC AND ORGANIC ACIDS, METHODS OF PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION BASED THEREON

机译:具有无机和有机酸的6- [X-(2-羟乙基)氨基烷基] -5,11-二氧代-5,6-二羟基-11H-茚满[1,2-C]异喹啉或盐,其制备方法,药物和药物成分

摘要

FIELD: medicine. SUBSTANCE: invention describes indeno [1,2-c]isoquinoline derivatives of formula I wherein X is the number of carbon atoms of 0-5 in aminoalkyl group. Indenoisoquinolines are prepared by reacting indeno [1,2-c] isocumarine and/or 1-methoxy-2- (2-methoxycabonylphenyl)-inden-3-one with N- (hydroxyethyl)alkylene diamine in aprotic solvent at elevated temperature. The other preparation method comprises reacting 6-(X-chloroalkyl)-5,11-dioxo-5,6- dihydro-11H-indeno [1,2-c] isoquinolines with 2- aminoethanol in the presence of anhydrous potassium carbonate in suitable solvent. Compounds of formula i have antitumor activity and are useful for preparation of agents for treating malignant tumors in mammals. EFFECT: improved properties of the pharmaceutical composition. 7 cl, 17 ex, 6 tbl
机译:领域:医学。物质:本发明描述了式I的茚并[1,2-c]异喹啉衍生物,其中X是氨基烷基中0-5的碳原子数。茚并异喹啉是通过使茚并[1,2-c]异豆香碱和/或1-甲氧基-2-(2-甲氧基羰基苯基)-茚满-3-酮与N-(羟乙基)亚烷基二胺在非质子溶剂中在高温下反应而制备的。另一种制备方法包括在合适的无水碳酸钾存在下,使6-(X-氯烷基)-5,11-二氧代-5,6-二氢-11H-茚并[1,2-c]异喹啉与2-氨基乙醇反应。溶剂。式I化合物具有抗肿瘤活性,可用于制备用于治疗哺乳动物恶性肿瘤的药剂。效果:改善了药物组合物的性能。 7 cl,17 ex,6汤匙

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