摘要
A method for the generation of alkyl radicals from inert alkyl C-o bonds has been developed via an iron/borane reagent/alkoxide catalytic system,which can be employed for the synthesis of amines from nitroarenes with excellent efficiency.This reductive amination features good functional group compatibility and enables the late-stage amination of bio-relevant compounds,thus providing good opportunities for applications in medicinal chemistry.Preliminary mechanistic studies reveal that the amine synthesis may be involving a Fe/Li cation-assisted single electron transfer pathway to form alkyl radicals,and the low-valent iron speciesmaybetheactive intermediates.
基金
the financial support from National Natural Science Foundation of China(Nos.22271031,22201026),Natural Science Foundation of Chongqing(No.CSTB2022NSCQ-MSX1065)
Chongqing Postdoctoral Science Foundation(No.cstc2020jcyj-bshX0052)
Medical Imaging Key Laboratory of Sichuan Province(Nos.MIKL202201 and MIKL202202)
Affiliated Hospital of North Sichuan Medical College(No.2022JB001)
Youth Project of Science and Technology Research Program of Chongqing Education Commission of China(No.KJQN201900112).
