A practical one-pot preparation of carbamoyl fluorides from easily obtained pyridine N-oxide,commercially available secondary amines and synthetically versatile difluorocarbene precursors(Ruppert-Prakash reagent or Ch...A practical one-pot preparation of carbamoyl fluorides from easily obtained pyridine N-oxide,commercially available secondary amines and synthetically versatile difluorocarbene precursors(Ruppert-Prakash reagent or Chen's reagent)was developed herein,which dexterously resorted to the oxidation of difluorocarbene by external pyridine N-oxide to produce the toxic and gaseous fluorophosgene in situ.Notable features of this method include nice functionality tolerance,late-stage modification of drug molecules and the recoveryand recycle of quinoline.展开更多
基金The authors gratefully acknowledge the financial support from the National Natural Science Foundation of China(grant no.22271151)and the Distinguished Youth Foundation of Jiangsu Province.
文摘A practical one-pot preparation of carbamoyl fluorides from easily obtained pyridine N-oxide,commercially available secondary amines and synthetically versatile difluorocarbene precursors(Ruppert-Prakash reagent or Chen's reagent)was developed herein,which dexterously resorted to the oxidation of difluorocarbene by external pyridine N-oxide to produce the toxic and gaseous fluorophosgene in situ.Notable features of this method include nice functionality tolerance,late-stage modification of drug molecules and the recoveryand recycle of quinoline.
