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    • 4. 发明授权
    • Novel organosilicon compounds and anti-transplanted tumor agents
containing the same
    • 新型有机硅化合物和含有其的抗移植肿瘤剂
    • US4278666A
    • 1981-07-14
    • US124957
    • 1980-02-26
    • Shigeshi ToyoshimaRyuichi SatoKoichi ItoToshio ShinoharaYasushi Yamamoto
    • Shigeshi ToyoshimaRyuichi SatoKoichi ItoToshio ShinoharaYasushi Yamamoto
    • A61K31/695A61P35/00C07F7/08C07F7/10A61K31/725A01N55/00
    • C07F7/0818
    • The invention provides a novel class of organosilicon compounds and a method for the preparation thereof as well as an anti-tumor agent containing the compound having very remarkable anti-tumor activity but with very low toxicity. The inventive compound is a (trihydrocarbylsilylmethyloxyimino)alkane, which is a silicon-containing oxime compound hitherto not described in any prior art literatures, represented by the general formula R.sup.1.sub.3 Si--CH.sub.2 --O--N.dbd.Y, R.sup.1 is a substituted or unsubstituted monovalent hydrocarbon group having from 1 to 10 carbon atoms and Y is a divalent hydrocarbon group denoted by .dbd.CR.sup.2 R.sup.3 or .dbd.CR.sup.4, R.sup.2 and R.sup.3, which may be identical or different, having the same meaning as R.sup.1 defined above and R.sup.4 being an alkylene group to form a ring structure jointly with the carbon atom directly bonded to the nitrogen atom. Typical examples of the compounds are: 2-(trimethylsilylmethyloxyimino) butane, 2-(trimethylsilylmethyloxyimino)propane, 2-(dimethylphenylsilylmethyloxyimino) butane and trimethylsilylmethyloxyiminocyclohexane.
    • 本发明提供了一类新颖的有机硅化合物及其制备方法以及含有非常显着的抗肿瘤活性但毒性非常低的化合物的抗肿瘤剂。 本发明化合物是一种(三烃基甲硅烷基甲氧基亚氨基)烷烃,其是迄今尚未在任何现有技术文献中描述的含硅肟化合物,由通式R 13 Si-CH 2 -ON A = Y表示,R 1是取代或未取代的单价烃基, 1至10个碳原子,Y是由= CR 2 R 3或= CR 4,R 2和R 3表示的二价烃基,其可以相同或不同,具有与上述R 1相同的含义,R 4为形成环的亚烷基 与与氮原子直接键合的碳原子结合。 化合物的典型实例是:2-(三甲基甲硅烷基甲氧基亚氨基)丁烷,2-(三甲基甲硅烷基甲氧基亚氨基)丙烷,2-(二甲基苯基甲硅烷基甲氧基亚氨基)丁烷和三甲基甲硅烷基甲氧基亚氨基环己烷。