Process for the manufacture of LH-RH and LH-RH analogs using Glu-His(DnP)-OH

摘要

What is disclosed is a method for the manufacture of LH-RH and LH-RH analogs, which comprises reacting Glu-His(DnP)-OH with the corresponding peptide having a free amino group and protected carboxy groups in a solvent as used in peptide chemistry and with the addition of 3-hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazine (HOObt) and a carbodiimide and then splitting off the Dnp-(2,4-dinitrophenyl) group. The new method greatly reduces the degree of histidine racemization. The invention also provides a new dipeptide, i.e. Glu-His(Dnp)-OH.