| abstract |
The invention discloses a preparation method and application of unactivated olefin hydrofluoromethylation, which comprises the following steps: A. adding non-activated olefin I, sodium trifluromethyl sulfinate and photocatalyst Ir [ dF (CF) into a schlenk tube 3 )ppy] 2 (dtbpy)PF 6 (ii) a B. Vacuumizing and changing argon, and adding methanol; C. irradiating a schlenk tube by a fluorescent lamp, and stirring for reaction; D. after the reaction is finished, adding water into the system to quench the reaction, extracting with ethyl acetate, separating out an organic phase, drying, filtering, performing rotary evaporation to remove the solvent, and performing column chromatography on the residue by using an ethyl acetate/petroleum ether mixed solvent to obtain a target product II, wherein the proportion of the ethyl acetate/petroleum ether mixed solvent is selected according to different polarities of the product, and the column chromatography adopts silica gel as a stationary phase. The use of the method in the synthesis of drug molecules. The method is easy to implement and simple and convenient to operate, and a cheap trifluoromethyl reagent is selected to realize the hydrogen trifluoromethylation reaction of the unactivated olefin under mild conditions to prepare a series of target compounds containing trifluoromethyl. |