- Practical one-pot C-H activation/borylation/oxidation: Preparation of 3-bromo-5-methylphenol on a multigram scale
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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.
- Norberg, A. Monica,Smith III, Milton R.,Maleczka Jr., Robert E.
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- COMPOUNDS AND METHODS OF PROMOTING MYELINATION
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The present invention relates to a method of promoting myelination of central nervous system neurons in a subject suffering from a myelin-related disorder, the method comprising administering to the subject a therapeutically effective amount of a compound
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- Structure-Based Approach to Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators
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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.
- 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
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p. 6451 - 6457
(2017/08/02)
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- Process for the synthesis of phenols from arenes
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A process to synthesize substituted phenols such as those of the general formula RR′R″Ar(OH) wherein R, R′, and R″ are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C—H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.
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- C-H activation/borylation/oxidation: A one-pot unified route to meta-substituted phenols bearing ortho-/para-directing groups
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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
- Maleczka Jr., Robert E.,Shi, Feng,Holmes, Daniel,Smith III, Milton R.
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p. 7792 - 7793
(2007/10/03)
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- Novel halogenated phenol esters, antimicrobial compositions containing them and their use
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Halogenated phenol esters of the formula STR1 wherein X represents chlorine or fluorine and R represents hydrogen, alkyl of 1 to 22 carbon atoms, alkenyl of 2 to 22 carbon atoms, benzyl which is unsubstituted or substituted by chlorine or bromine atoms, o
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