A coupling reagent that causes very little epimerization and is good for large scale synthesis and PNA synthesis.1 In the coupling of peptide fragments to form SK&F 107647, TDBTU was shown to produce significantly less epimerization than PyBOP, HBTU, HATU, and many other common coupling reagents.2,3 TDBTU was utilized in the large scale synthesis of over 2 kg of SK&F 107647.2
1. Org. Prep. Proced. Int. 2001, 33, 203.
2. J. Peptide Res. 1999, 54, 54.
3. Tetrahedron 2004, 60, 2447.