在我们对烷基膦酸酯的修改工作的基础1,一系列α-(取代的phenoxybutyryloxy或戊酰氧基)烷基膦酸酯(4 - 5)和2-(取代的phenoxybutyryloxy)烷基-5,5-二甲基-1,3,2-设计并合成了-dioxaphosphinan-2-one(6)。生物测定结果表明,在150 g ai / ha下,14种标题化合物4表现出明显的苗后除草活性,对草皮,普通mar菜和假雏菊有活性。化合物5对所有测试的杂草均无活性。化合物6对被测双子叶杂草表现出中等至良好的抑制作用。结构-活性关系(SAR)分析表明,作为连接桥的碳链长度对除草活性有很大影响。化合物的广谱测试4-1,4-2,4-9,4-30,和4-36在75克活性成分/公顷下进行。特别是4-1对被测双子叶杂草表现出100%的抑制活性,高于草甘膦。
[EN] PYRAZOLOQUINAZOLINONE ANTITUMOR AGENTS<br/>[FR] AGENTS ANTITUMORAUX À BASE DE PYRAZOLOQUINAZOLINONE
申请人:KAPOOR TARUN M
公开号:WO2018213712A1
公开(公告)日:2018-11-22
Compounds of formula: (I) (II) are useful as antitumor agents. In these compounds, R10 is (a) (C1-C10) hydrocarbyl, (C1-C10)halohydrocarbyl, (C1-C6)hydroxyalkyl, or (III) or R10 is (b), (IV) in which Q and A are linkers and Ar is optionally substituted monocyclic or bicyclic aryl or heteroaryl.
Compounds of formula:
are useful as antitumor agents. In these compounds, R10 is (a) (C1-C10) hydrocarbyl, (C1-C10)halohydrocarbyl, (C1-C6)hydroxyalkyl, or
or R10 is (b)
in which Q and A are linkers and Ar is optionally substituted monocyclic or bicyclic aryl or heteroaryl.