- Beta-trifluoromethyl vinyl sulfone compounds as well as preparation method and application thereof
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The invention belongs to the technical field of organic compounds and particularly provides beta-trifluoromethyl vinyl sulfone compounds, a preparation method thereof and an application of the compounds to tumor cell proliferation resistance. The beta-trifluoromethyl vinyl sulfone compounds are prepared from a multicomponent reagent (trifluoromethyl) trimethylsilane (TMSCF3), alkyne, diazonium salt and DABCO.(SO2)2 in an organic solvent DMSO through a one-step reaction. Reaction conditions are quite mild, alkyne bi-functionalization is realized directly through the one-step cascade reaction of the four raw materials, the operation is simple, defects of tedious steps, low operability and yield and poor selectivity of the traditional synthesis method of vinyl sulfone derivatives are overcome, and the method is applicable to large-scale preparation and has quite good application prospect. In-vitro pharmacological activity screening tests show that the compounds have an anti-proliferation effect on tumor cells, part of the compounds have an obvious tumor inhibition activity, the half maximal inhibitory concentration IC50 value can reach mu m level, and the compounds can be used for preparing a kind of novel anti-tumor reagents.
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Paragraph 0025-0027; 0054
(2018/03/24)
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- HALOALKYL HETEROARYL BENZAMIDE COMPOUNDS
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A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
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Page/Page column 129-130
(2010/12/17)
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- Regio- and stereo-selective synthesis of trifluoromethylated isoxazolidines by 1,3-dipolar cycloaddition of 1,1,1-trifluoro-3-phenylsulfonylpropene with nitrones, and their conversion into trifluoromethylated syn-3-amino alcohols
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1,1,1-Trifluoro-3-phenylsulfonylpropene 1, a useful synthetic precursor for trifluoromethylated compounds, has been prepared from methyl phenyl sulfone 2 and ethyl trifluoroacetate.The 1,3-dipolar cycloaddition of 1 with various nitrones 5a-f gave 5-trifl
- Tsuge, Hiroyasu,Okano, Takashi,Eguchi, Shoji
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p. 2761 - 2766
(2007/10/02)
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