On October 16, 2008, Beaton, Graham; Chen, Mi; Coon, Timothy Richard; Ewing, Todd; Jiang, Wanlong; Lowe, Richard; Moree, Willy; Smith, Nicole; Wade, Warren; Zhao, Liren; Zhu, Yun-Fei; Rowbottom, Martin; Ashweek, Neil published a patent.Synthetic Route of 156267-13-9 The title of the patent was Preparation of benzenecarboxamide derivatives as Gonadotropin-releasing hormone receptor antagonists. And the patent contained the following:
Title compounds represented by the formula I [wherein A = pyridyl, Ph, quinolinyl, etc.; R1a = H, halo, alkyl, etc.; R1b, R1c = independently H, halo, OH, etc.; R1d = F, Cl, Me, CF3 or cyano; R2 = alkyl-(R5)p; R2a = (un)substituted Ph, (hetero)aryl or alkyl; R5 = independently H, OH, amino, etc.; p = 1-3; and stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof] were prepared as Gonadotropin-releasing hormone receptor (GnRH) antagonists. For example, II was provided in a multi-step synthesis starting from 3-bromo-4-chlorobenzoic acid. I were tested in one or more of the peptide competitive human receptor binding assays and showed Ki values of 1 μM or less. Thus, I and their pharmaceutical compositions are useful for the treatment of a variety of sex-hormone related conditions in both men and women. The experimental process involved the reaction of N,3-Dimethylpyridin-2-amine(cas: 156267-13-9).Synthetic Route of 156267-13-9
The Article related to benzenecarboxamide pyridinyl preparation gonadotropin releasing hormone receptor antagonist, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Synthetic Route of 156267-13-9