Difluorocarbene-Promoted Condensation of Primary Amine and Tertiary Amine to Prepare Amidines
This research aimed to explore a green and efficient method for the synthesis of amidines.A series of amidines were synthesized by one-pot method from aromatic amine,sodium chlorodifluoroacetate and triethylamine and the optimal reaction conditions were determined by optimizing the solvent,difluoro-carbene source,time,temperature and material ratio;the reaction temperature was 100℃,the reaction time was 12 h,anhydrous acetonitrile was used as the solvent,and the material ratio n(aromatic amine)∶n(sodium chlorodifluoroacetate)∶n(triethylamine)was 1∶2∶3.The finding showed the yield was in-creased by 28%compared with that before the optimization,the substrate was extended under the reaction conditions,and the amidine derivatives with a yield of 48%-65%were obtained.
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