During the synthesis of peptide nucleic acid (PNA) analogues, HATU was successfully used as a coupling reagent along with collidine, both in solution and solid phase. Furthermore, the synthetic route towards dehydrodidemnin B was improved by the use of HATU.
Current methods towards their synthesis frequently rely on the use of dipolar aprotic solvents; however, due to increasingly stringent regulations and growing societal pressures, safe and more sustainable alternatives are highly sought after.
HATU(1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxid hexafluorophosphate) is a reagent used inpeptide couplingchemistry to generate an active ester from a carboxylic acid. HATU can be used along with Hünig's base(N,N-diisopropylethylamine, DIPEA) to form amide bonds.
A mide bonds are one of the underpinning linkages in all living systems and are fundamental within drug discovery.
