4837-17-6Relevant academic research and scientific papers
Preparation method of difluoromethyl sulfone compound
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Paragraph 0134-0136, (2021/03/31)
The invention discloses a preparation method of a difluoromethyl sulfone compound. The invention provides a preparation method of a difluoromethyl sulfone compound, which comprises the following step:in a solvent, in the presence of alkali and a phase transfer catalyst, carrying out difluoromethylation reaction shown in the specification on sulfinic acid and/or salt thereof and CHClF2 to obtain the difluoromethyl sulfone compound. The solvent is a mixed solvent of water and an organic solvent; The sulfinic acid and/or salt thereof comprises positive ions and negative ions, and the negative ions contain structural fragments shown as a formula I; and the difluoromethyl sulfone compound contains a structural fragment as shown in a formula II which is described in the specification. The preparation method provided by the invention has the advantages of accessible raw materials, wide substrate range, mild reaction conditions and simple operation, can implement separation without column chromatography, and is suitable for industrial production. The difluoromethyl sulfone compound can be obtained at a high yield.
Copper-Mediated Di- and Monofluoromethanesulfonylation of Arenediazonium Tetrafluoroborates: Probing the Fluorine Effect
Xing, Bo,Ni, Chuanfa,Hu, Jinbo
, p. 206 - 212 (2018/02/06)
A copper-mediated di- and monofluoromethanesulfonylation of arenediazonium tetrafluoroborates using di- and monofluoromethanesulfinate reagents provides aryl difluoromethyl (or monofluoromethyl) sulfones in good yields. It was found that the relative reactivity of these sodium fluoroalkanesulfinates in the present reactions decreases in the following order: CH2FSO2Na > CF2HSO2Na > CF3SO2Na.
Conversion of methyl ketones and methyl sulfones into α-deutero-α,α-difluoromethyl ketones and α-deutero-α,α-difluoromethyl sulfones in three synthetic steps
Sowaileh, Munia F.,Han, Changho,Hazlitt, Robert A.,Kim, Eun Hoo,John, Jinu P.,Colby, David A.
supporting information, p. 396 - 400 (2017/01/10)
Deuterodifluoromethyl ketones and sulfones were assembled in three synthetic steps from methyl ketones and sulfones, respectively. The key synthetic transformation is the deuteration of the difluorocarbanion generated by the release of trifluoroacetate from highly α-fluorinated gem-diols. High levels of deuterium on the “CF2D” group were routinely observed. This strategy is mild and versatile and it can be applied to both ketones and sulfones without additional concerns of over- or under-fluorination. Additional examples address issues of over-deuteration when compounds with other acidic protons are subjected to the reaction conditions. This process not only demonstrates a new method to install a “CF2D” group but also extends the scope of trifluoroacetate release to sulfones.
Difluoromethylation of: N -arylsulfonyl hydrazones with difluorocarbene leading to difluoromethyl aryl sulfones
Zheng, Qu-Tong,Wei, Yun,Zheng, Jian,Duan, Ya-Ya,Zhao, Gang,Wang, Zong-Bao,Lin, Jin-Hong,Zheng, Xing,Xiao, Ji-Chang
, p. 82298 - 82300 (2016/09/09)
The difluoromethylation of N-arylsulfonyl hydrazones with difluorocarbene generated from difluoromethylene phosphobetaine (Ph3P+CF2CO2-) to give various difluoromethyl aryl sulfones is described.
