757247-59-9Relevant academic research and scientific papers
Electrocatalytic generation of amidyl radicals for olefin hydroamidation: Use of solvent effects to enable anilide oxidation
Zhu, Lin,Xiong, Peng,Mao, Zhong-Yi,Wang, Yong-Heng,Yan, Xiaomei,Lu, Xin,Xu, Hai-Chao
, p. 2226 - 2229 (2016/02/19)
Oxidative generation of synthetically important amidyl radicals from N-H amides is an appealing and yet challenging task. Previous methods require a stoichiometric amount of a strong oxidant and/or a costly noble-metal catalyst. We report herein the first electrocatalytic method that employs ferrocene (Fc), a cheap organometallic reagent, as the redox catalyst to produce amidyl radicals from N-aryl amides. Based on this radical-generating method, an efficient intramolecular olefin hydroamidation reaction has been developed. Easy access to N-arylamidyl radicals: The first electrocatalytic method for the generation of amidyl radicals from anilides has been developed using ferrocene (Cp2Fe) as a highly reactive, yet chemoselective redox catalyst. Based on this radical-generating method, a highly chemo- and diastereoselective olefin hydroamidation reaction has been developed.
Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications
Li, James J.,Sutton, James C.,Nirschl, Alexandra,Zou, Yan,Wang, Haixia,Sun, Chongqing,Pi, Zulan,Johnson, Rebecca,Krystek Jr., Stanley R.,Seethala, Ramakrishna,Golla, Rajasree,Sleph, Paul G.,Beehler, Blake C.,Grover, Gary J.,Fura, Aberra,Vyas, Viral P.,Li, Cindy Y.,Gougoutas, Jack Z.,Galella, Michael A.,Zahler, Robert,Ostrowski, Jacek,Hamann, Lawrence G.
, p. 3015 - 3025 (2008/02/06)
A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active and muscle selective androgen receptor modulators (SARMs), with most of the compounds exhibiting low nM in vitro potency in androgen receptor (AR) binding and functional assays. Once daily oral treatment with the lead compound 11a (AR Ki = 0.9 nM, EC50 = 1.8 nM) for 14 days induced muscle growth with an ED50 of 0.09 mg/kg, providing approximately 50-fold selectivity over prostate growth in an orchidectomized rat model. Pharmacokinetic studies in rats demonstrated that the lead compound 11a had oral bioavailability of 65% and a plasma half-life of 5.5 h. On the basis of their preclinical profiles, the SARMs in this series are expected to provide beneficial anabolic effects on muscle with minimal androgenic effects on prostate tissue.
