Making chloroethylamino-substituted derivatives of aminoalkyl esters of indole-carboxylic acid, having antitumor activity involves e.g. reacting ethyl-bromo-(bromomethyl)-methoxy-methyl-1H-indole-carboxylate with bis(chloroethyl)amine
2024-09-20
专利权人FEDERAL STATE BUDGETARY INST (FSBI-C)
申请日期2024-09-20
专利号RU2024127831-A
成果简介NOVELTY - Obtaining chloroethylamino-substituted derivatives of aminoalkyl esters of indole-3-carboxylic acid i.e. 1-methyl-2-[di(2-chloroethyl)aminomethyl]-3-carbethoxy-5-methoxy-6-bromoindole (I) and 1-cyclohexyl-2-[di(2-chloroethyl)aminomethyl]-3-carbethoxy-5-methoxy-6-bromoindole (II) as active agent possessing antitumor activity. USE - The method is useful for obtaining chloroethylamino-substituted derivatives of aminoalkyl esters of indole-3-carboxylic acid, possessing antitumor activity. No biological data given. ADVANTAGE - The method produces chloroethylamino-substituted derivatives of aminoalkyl esters of indole-3-carboxylic acid which is stable and upon parenteral administration inhibits the growth of neoplasms of many histogenesis, without inducing significant negative toxic effects. DETAILED DESCRIPTION - Obtaining chloroethylamino-substituted derivatives of aminoalkyl esters of indole-3-carboxylic acid i.e. 1-methyl-2-[di(2-chloroethyl)aminomethyl]-3-carbethoxy-5-methoxy-6-bromoindole of formula (I) and 1-cyclohexyl-2-[di(2-chloroethyl)aminomethyl]-3-carbethoxy-5-methoxy-6-bromoindole of formula (II) as active agent possessing antitumor activity, comprises (a) reacting ethyl 5-hydroxy-1,2-dimethyl-1H-indole-3-carboxylate of formula (III) to obtain ethyl 5-methoxy-1,2-dimethyl-1H-indole-3-carboxylate of formula (IV), (b) reacting (IV) to obtain ethyl 6-bromo-5-methoxy-1,2-dimethyl-1H-indole-3-carboxylate of formula (V), reacting (V) to obtain ethyl 6-bromo-2-(bromomethyl)-5-methoxy-1-methyl-1H-indole-3-carboxylate of formula (VI), and (c) reacting (VI) in the presence of bis(2-chloroethyl)amine to obtain (I).
IPC 分类号C07D-209/42
国家俄罗斯
专业领域化学化工
语种英语
成果类型专利
文献类型科技成果
条目标识符http://119.78.100.226:8889/handle/3KE4DYBR/15096
专题中国科学院新疆生态与地理研究所
作者单位
FEDERAL STATE BUDGETARY INST (FSBI-C)
推荐引用方式
GB/T 7714
FILIMONOVA M V,SOLDATOVA O V,SURINOVA V I,et al. Making chloroethylamino-substituted derivatives of aminoalkyl esters of indole-carboxylic acid, having antitumor activity involves e.g. reacting ethyl-bromo-(bromomethyl)-methoxy-methyl-1H-indole-carboxylate with bis(chloroethyl)amine. RU2024127831-A[P]. 2024.
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