Author/Authors :
Ralf Wischnat، نويسنده , , Ralf and Rudolph، نويسنده , , Joachim and Hanke، نويسنده , , Roman and Kaese، نويسنده , , Roger and May، نويسنده , , Achim and Theis، نويسنده , , Heidi and Zuther، نويسنده , , Undine، نويسنده ,
Abstract :
An efficient scalable synthesis of 2-halothiazolium-type peptide coupling reagents has been developed. The key step is the formation of the 2-bromothiazole scaffold through cyclization of α-thiocyanato ketones with hydrogen bromide. Using this method, the new coupling reagent 2-bromo-N-methylthiazolium bromide (BMTB) was synthesized. BMTB was tested in a difficult model coupling reaction of two sterically hindered N-methylated amino acids and showed higher activity than the well-established peptide coupling reagent HATU.
