1940-28-9Relevant articles and documents
Practical one-pot C-H activation/borylation/oxidation: Preparation of 3-bromo-5-methylphenol on a multigram scale
Norberg, A. Monica,Smith III, Milton R.,Maleczka Jr., Robert E.
, p. 857 - 859 (2011)
A practical one-pot C-H activation/borylation/oxidation sequence for the generation of 3,5-disubstituted phenols is presented. Specifically, 3-bromo-5-methylphenol is prepared from 3-bromotoluene, without isolation of intermediates, on a multigram scale, and in high yield. The process proceeds under mild conditions and can be completed within one day. Georg Thieme Verlag Stuttgart - New York.
Structure-Based Approach to Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators
Unwalla, Ray,Mousseau, James J.,Fadeyi, Olugbeminiyi O.,Choi, Chulho,Parris, Kevin,Hu, Baihua,Kenney, Thomas,Chippari, Susan,McNally, Christopher,Vishwanathan, Karthick,Kilbourne, Edward,Thompson, Catherine,Nagpal, Sunil,Wrobel, Jay,Yudt, Matthew,Morris, Carl A.,Powell, Dennis,Gilbert, Adam M.,Chekler, Eugene L. Piatnitski
, p. 6451 - 6457 (2017/08/02)
In an effort to find new and safer treatments for osteoporosis and frailty, we describe a novel series of selective androgen receptor modulators (SARMs). Using a structure-based approach, we identified compound 7, a potent AR (ARE EC50 = 0.34 nM) and selective (N/C interaction EC50 = 1206 nM) modulator. In vivo data, an AR LBD X-ray structure of 7, and further insights from modeling studies of ligand receptor interactions are also presented.
C-H activation/borylation/oxidation: A one-pot unified route to meta-substituted phenols bearing ortho-/para-directing groups
Maleczka Jr., Robert E.,Shi, Feng,Holmes, Daniel,Smith III, Milton R.
, p. 7792 - 7793 (2007/10/03)
An efficient one-pot C-H activation/borylation/oxidation protocol for the preparation of phenols is described. This method is particularly attractive for the generation of meta-substituted phenols bearing ortho-/para-directing groups, as such substrates are difficult to access by other phenol syntheses. Copyright