PROCESS FOR THE PREPARATION OF LH-RH OR LH-RH ANALOGS

摘要

LH-releasing hormone, pyroGlu-His-Trp-Ser-Tyr-Gly-Leu-ArgPro-Gly-NH2 (I), and its analogs were prepd. by coupling pyroGlu-His(Dnp)-OH [Dnp = 2,4-dinitrophenyl with the appropriate peptide-free amine by a carbodiimide in thre presence of 3-hydroxy-4-oxo-3,4-dihydro-1,2,3- benzotriazine (HOBt), and cleaving the Dnp group from the resulting protected peptide with NH2NH2 or a thiol. Thus, pyroGlu-His-OH was treated with 2,4-dinitrofluorobenzene to give II, which was coupled to H-TrpGly-Leu-Arg-Pro-Gly-NH by DCC/HOBt to give the protected decapeptide amide, which was Dnp-deblocked by NH2NH2 to give I.