Buchwald-Hartwig Amination-A Modern Technology for the Synthesis of Intermediates and APIs

摘要

The vast majority of active pharmaceutical ingredients (APIs) and thus also many of the intermediates of these compounds contain a nitrogen moiety.This structural feature may serve as a basic core,may influence the physical properties such as solubility or polarity,and may be the pharmacophore for biological activity in itself.In many cases,these motifs are derived from diversely substituted anilines.From a synthetic point of view,the retrosynthetic strategy apart from well known techniques such as nitro group reduction or reductive amination is the direct build-up of the desired C-N bond.