- Pd-Catalyzed Decarboxylative Ortho-Halogenation of Aryl Carboxylic Acids with Sodium Halide NaX Using Carboxyl as a Traceless Directing Group
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A highly regioselective Pd-catalyzed carboxyl directed decarboxylative ortho-C-H halogenation of cheap o-nitrobenzoic acids with NaX (X = I, Br) under aerobic conditions has been established. The utility of the method has been demonstrated by the gram-scale reaction and derivatization of the product. Experimental results have confirmed Pd and Bi played critical roles in the transformation and indicated the transformation might proceed via 2-halo-6-nitrobenzoic acid derivative intermediate.
- Fu, Zhengjiang,Jiang, Yongqing,Wang, Shuiliang,Song, Yuanyuan,Guo, Shengmei,Cai, Hu
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supporting information
p. 3003 - 3007
(2019/05/10)
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- Method for synthesizing m-iodonitrobenzene compound
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Provided is a method for synthesizing m-iodonitrobenzene; in the presence of oxygen gas, a palladium catalyst, a copper additive, a bismuth reagent and potassium phosphate, an o-nitrobenzoic acid compound and metal iodide are subjected to a substitution reaction in an organic solvent to form a corresponding m-iodonitrobenzene compound, wherein a metal in the metal iodide is an alkali metal or an alkaline earth metal. The method has obvious advantages of cheap and easily obtained reaction raw materials (including o-nitrobenzoic acid and MI), small amount of the metal catalyst, minimum environmental pollution with oxygen gas as an oxidant, good tolerance on various functional groups on an aromatic ring and the like. The method can be widely applied in the fields of synthesis of drugs, materials, natural products and the like in industrial and academic circles.
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Paragraph 0057-0058
(2018/03/24)
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- Steroid receptor modulator compounds and methods
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- Tricyclic steroid receptor modulator compounds and methods
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- Steroid receptor modulator compounds and methods
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiting steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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