33709-38-5Relevant academic research and scientific papers
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: Optimization of the tryptamine side chain
Young, Jonathan R.,Huang, Song X.,Walsh, Thomas F.,Wyvratt Jr., Matthew J.,Yang, Yi Tien,Yudkovitz, Joel B.,Cui, Jisong,Mount, George R.,Ren, Rena Ning,Wu, Tsuei-Ju,Shen, Xiaolan,Lyons, Kathryn A.,Mao, An-Hua,Carlin, Josephine R.,Karanam, Bindhu V.,Vincent, Stella H.,Cheng, Kang,Goulet, Mark T.
, p. 827 - 832 (2007/10/03)
A series of 2-arylindoles containing novel heteroaromatic substituents on the tryptamine tether, based on compound 1, was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. Successful modifications of 1 included chain length variation (reduction) and replacement of the pyridine with heteroaromatic groups. These alterations culminated in the discovery of compound 27kk which had excellent in vitro potency and oral efficacy in rodents.
A USEFUL METHOD FOR SELECTIVE ACYLATION OF ALCOHOLS USING 2,2'-BIPYRIDYL-6-YL CARBOXYLATE AND CESIUM FLUORIDE
Mukaiyama, Teruaki,Pai, Fong-Chang,Onaka, Makoto,Narasaka, Koichi
, p. 563 - 566 (2007/10/02)
Primary and secondary alcohols are acylated under mild conditions by the of use 2,2'-bipyridyl-6-yl carboxylates and cesium fluoride.Furthermore, the reaction is successfully applied to selective acylation of a primary carbinol group of diols containing primary and secondary carbinol groups or exclusive O-acylation of aromatic amino alcohols.
