312-21-0Relevant articles and documents
Method for constructing fluorine-containing methyl sulfone compound through multi-component coupling
-
Paragraph 0171-0174, (2021/10/27)
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.
Practical and efficient synthesis of aryl trifluoromethyl sulfones from arylsulfonyl chlorides with Umemoto's reagent II
Zhou, Xiaocong,Hu, Dufen,He, Xinyi,Li, Yuanqiang,Chu, Youqun,She, Yuanbin
supporting information, (2019/12/24)
A practical and efficient method for the synthesis of aryl trifluoromethyl sulfones has been developed by a tandem reaction of arylsulfonyl chlorides with Umemoto's reagent II. The advantageous features of this method are simple operation, mild reaction conditions, wide scope of substrates, high yield of products, and easy scalability.
Copper-Promoted Trifluoromethanesulfonylation and Trifluoromethylation of Arenediazonium Tetrafluoroborates with NaSO2CF3
Zhang, Ke,Xu, Xiu-Hua,Qing, Feng-Ling
, p. 7658 - 7665 (2015/08/18)
A tunable chemoselective trifluoromethanesulfonylation and trifluoromethylation of arenediazonium tetrafluoroborates with Langlois' reagent (NaSO2CF3) was developed. The Cu2O-catalyzed reaction in DMSO gave aryl trifluoromethanesulfones as the major products. On the other hand, the trifluoromethylated arenes were produced in the presence of oxidant tert-butyl hydroperoxide, CuBF4(MeCN)4, and 2,2′;6′,2 terpyridine (tpy). Both of these transformations proceed under mild conditions and tolerate functional groups.
