Boronic acids are recognized as useful scaffolds for pharmaceutical compounds, due to their unique property of forming a reversible covalent bond at the boron center with various nucleophilic functional groups. Particularly, benzoxaboroles have gathered much interest as a boron-containing scaffold for bioactive compounds with unique mechanisms of action.

In drug discovery research, sp³-carbon-rich compounds with low planarity are gathering more attention in order to improve off-target effects and lipophilicity. These three compounds [M3627],[M3633],[B6525] with electron-rich di(2-picolyl)amine moieties are available as ligands for nickel-catalyzed C(sp²)-C(sp³) cross-coupling. Please also refer TCI product spotlight. 

The ligand [D6165] forms cobalt complexes to catalyze meta-selective C-H borylation of fluorobenzenes. D6165 allows the synthesis of building blocks that are inaccessible by conventional methods and is expected to advance various pharmaceutical intermediate synthesis studies.

We are proud to present the synthesis of 4-bromobenzonitrile by the dehydration reaction of 4-bromobenzamide using trifluoromethanesulfonic anhydride [T1100].