Gonadotropin-releasing hormone antagonists: novel members of the azaline B family

JE Rivier, G Jiang, J Porter, C Hoeger…

Index: Rivier, Jean E.; Jiang, Guangcheng; Porter, John; Hoeger, Carl A.; Craig, A. Grey; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 14 p. 2649 - 2662

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Citation Number: 61

Abstract

GnRH). Introduction of either mesityl,(2-~ hlorophenyl) isourrea, or (3-chloropheny1) isouea as a substituent on the 4-amino function at residues 5 and 6 of the azaline B precursor was considerably less successful. In this article, we describe in details, improved synthetic protocols for all novel amino acis, Na-methylation of amino acids on the resin, and elimination of the undesired Nfu-methylation of pyridylalanine at position 3 as the result of ...