Among the various fluorinated moieties(especially lightly-fluorinated-groups), the difluoromethyl group(-CF2H) has recently garned much more attention in the areas of drug, agrochemical and material research beacuse it can act as a more lipohilic isostere of carbinol, thiol,hydroxmaic acid or amide groups.Representative pharmaceuticals and agrochemicals that contain a difluoromethyl group include: Roflumilast(drug for COPD,chronic obstructive pulmonary disease),Fluxapyroxad(fungicide), Thiazopyr(herbicide),Inhibitor of cyclooxygenases and 5-lipoxygenase(anti-inflammatory agent),etc..
Difluoromethylated compounds are conventionally prepared through the deoxyfluorination of aldehydes with sulfur tetrafluoride(SF4),N,N-diethylaminosulfur trifluoride(DAST,kumi3F13)),bis(2-methoxyethyl)aminosulfur trifluoride(Deoxo-Fluor,kumi3F14) and other related reagents. However, the limitations of these methods,such as the need for harsh reaction conditions and poor functional-group tolerance, have restricted their wide utilization. Compared to the highly developed for trifluoromethylation, difluoromethylation is still remaining great challenges, probably due to the lack of efficient sources of the difluoromethyl group and stable difluoromethyl-metal complexes.
Our product catalogue has wide choices and novel sources for incorporating the difluoromethyl group into organic molecules through nucleophilic,electrophilic( involving difluorocarbene intermediates) and radical fluorination methods. For examples, typical nucleophilic difluoromethylation of carbonyls and imines is using (Difluoromethyl)trimethylsilane(kumi2F24) and Difluoromethyl phenyl sulfone(kumi2F25),developped by Jinbo Hu and coworkers. Both Zinc difluoromethanesulfinate (DFMS,kumi4F01) and Sodium difluoromethanesulfinate are crystalline,bench-top stable and broad functional group tolerant reagents for directly adding CF2H to target compounds in a radical process and a innovative pathway.As an additive-free and neutral difluorocarbene precursor developed by Xiao and coworkers, Difluoromethylenephosphobetaine(kumi2F03) is expect to find new and effective applications in the difluoromethylation of heteroatoms.
Difluoromethylating Reagents Overview
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You can either buy our difluoromethylating reagents and then introduce difluoromethylated moiety into your own desired compounds, or you can simply order the building blocks pre-loaded with a -CF2H subsitituent.
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