C–H activation reactions as useful tools for medicinal chemists

• Published in: Bioorganic & medicinal chemistry letters 2016-11, Vol.26 (22), p.5378-5383
• Main Authors: Caro-Diaz, Eduardo J.E., Urbano, Mariangela, Buzard, Daniel J., Jones, Robert M.
• Format: Article
• Language: English
• Subjects: Catalysis; Chemistry Techniques, Synthetic - methods; Chemistry, Pharmaceutical - methods; C–H activation; Drug discovery; Drug Discovery - methods; Heterocycles; Heterocyclic Compounds - chemical synthesis; Heterocyclic Compounds - chemistry; Hydrocarbons, Aromatic - chemical synthesis; Hydrocarbons, Aromatic - chemistry; Medicinal chemistry; Pharmaceutical Preparations - chemical synthesis; Pharmaceutical Preparations - chemistry; Pharmaceuticals
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2016.06.036

[Display omitted] In recent years, there has been an exponential rise in the number of reports describing synthetic methods that utilize catalytic sp3 and sp2 C–H bond activation. Many have emerged as powerful synthetic tools for accessing biologically active motifs. Indeed, application to C–C and C–heteroatom bond formation, provides new directives for the construction of new pharmaceutical entities. Herein, we highlight some recent novel C–H activation processes that exemplify the utility of these transformations in medicinal chemistry.