- Method for constructing fluorine-containing methyl sulfone compound through multi-component coupling
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The invention discloses a fluorine-containing methyl sulfone compound as shown in a formula (1) and a synthesis method thereof. Aromatic iodide (aryl iodide or heteroaryl iodide), an inorganic sulfur reagent and a fluorine-containing building block are used as reaction raw materials and react in a solvent under the action of alkali, a catalyst and an additive to obtain a series of fluorine-containing methyl sulfone compounds. According to the invention, the fluorine-containing sulfone compound is constructed by a one-pot two-step method by taking an inorganic sulfur reagent as a sulfur source under a catalytic condition, so that the defects of the traditional synthesis of a fluorine-containing sulfone compound by thioether oxidation are avoided. According to the synthesis strategy developed by the invention, some clinical methyl sulfone drugs can be modified, and monofluoro, difluoro and trifluoromethyl sulfone compounds can be successfully obtained, which have huge potential in the field of drug development in the future.
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Paragraph 0121-0124
(2021/10/27)
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- Preparation method of difluoromethyl sulfone compound
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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.
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Paragraph 0130-0133
(2021/03/31)
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- Efficient asymmetric synthesis of aryl difluoromethyl sulfoxides and their use to access enantiopure α-difluoromethyl alcohols
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The -CHF2 moiety has shown a growing interest in pharmaceutical and agrochemical applications over the last few years. Its introduction is therefore a current research topic for organic chemists. Several groups have reported the synthesis of di
- Batisse, Chloé,Céspedes Dávila, Maria F.,Castello, Marco,Messara, Amélia,Vivet, Bertrand,Marciniak, Gilbert,Panossian, Armen,Hanquet, Gilles,Leroux, Frédéric R.
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p. 3063 - 3079
(2019/05/07)
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- Copper-Mediated Di- and Monofluoromethanesulfonylation of Arenediazonium Tetrafluoroborates: Probing the Fluorine Effect
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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.
- Xing, Bo,Ni, Chuanfa,Hu, Jinbo
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p. 206 - 212
(2018/02/06)
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- Difluoromethylation of: N -arylsulfonyl hydrazones with difluorocarbene leading to difluoromethyl aryl sulfones
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The difluoromethylation of N-arylsulfonyl hydrazones with difluorocarbene generated from difluoromethylene phosphobetaine (Ph3P+CF2CO2-) to give various difluoromethyl aryl sulfones is described.
- Zheng, Qu-Tong,Wei, Yun,Zheng, Jian,Duan, Ya-Ya,Zhao, Gang,Wang, Zong-Bao,Lin, Jin-Hong,Zheng, Xing,Xiao, Ji-Chang
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p. 82298 - 82300
(2016/09/09)
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