69172-21-0Relevant articles and documents
An efficient process for the synthesis of γ-arylbutanals via copper-mediated Grignard coupling
Monte, William T.,Lindbeck, Aline C.
, p. 267 - 269 (2001)
Copper-mediated Grignard cross-coupling of β-bromoethylene acetals with substituted benzyl halides can be combined with hydrolytic deprotection for an efficient and practical scale-up process to form γ-arylbutanals.
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.