192182-22-2Relevant academic research and scientific papers
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles
Chu, Lin,Hutchins, Jennifer E.,Weber, Ann E.,Lo, Jane-Ling,Yang, Yi-Tien,Cheng, Kang,Smith, Roy G.,Fisher, Michael H.,Wyvratt, Matthew J.,Goulet, Mark T.
, p. 509 - 513 (2007/10/03)
A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.
Synthesis of 2-aryltryptamines with palladium catalyzed cross-coupling of 2-bromotryptamines and arylboronic acids
Chu, Lin,Fisher, Michael H.,Goulet, Mark T.,Wyvratt, Matthew J.
, p. 3871 - 3874 (2007/10/03)
A versatile and high-yielding synthesis of 2-aryltryptamines employing palladium(0) catalyzed cross-coupling of 2-bromotryptamines and arylboronic acids was developed. The preparation of the intermediate 2-bromotryptamines with pyridine hydrobromide perbromide as the brominating agent, is also reported.
