- Metal-Free Aerobic Oxidation of Nitro-Substituted Alkylarenes to Carboxylic Acids or Benzyl Alcohols Promoted by NaOH
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Efficient and selective aerobic oxidation of nitro-substituted alkylarenes to functional compounds is a fundamental process that remains a challenge. Here, we report a metal-free, efficient, and practical approach for the direct and selective aerobic oxidation of nitro-substituted alkylarenes to carboxylic acids or benzyl alcohols. This sustainable system uses O2 as clean oxidant in a cheap and green NaOH/EtOH mixture. The position and type of substituent critically affect the products. In addition, this sustainable protocol enabled gram-scale preparation of carboxylic acid and benzyl alcohol derivatives with high chemoselectivities. Finally, the reactions can be conducted in a pressure reactor, which can conserve oxygen and prevent solvent loss. The approach was conducive to environmental protection and potential industrial application.
- Fang, Kun,Li, Guijie,She, Yuanbin
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p. 8092 - 8103
(2018/06/25)
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- Method for preparing nitro aromatic acid/nitro alpha-aryl alcohol through oxidizing substituted alkyl nitrobenzene by oxygen
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A method for preparing nitro aromatic acid/nitro alpha-aryl alcohol through oxidizing substituted alkyl nitrobenzene by oxygen comprises the following steps: taking substituted alkyl nitrobenzene shown as the formula (1) as a raw material, oxygen as an oxidizing agent and sodium hydroxide as an alkaline substance, mixing in a solvent uniformly, reacting for 3 to 24h at the temperature of 25 to 65 DEG C, and treating obtained reaction liquid to obtain the nitro aromatic acid or nitro alpha-aryl alcohol; the mass ratio of the substituted alkyl nitrobenzene to the sodium hydroxide is 1 to (2 to 10) and the oxygen pressure is 0.1 to 2.0 MPa. The method provided by the invention has the advantages that a catalyst is not needed, the raw material is low in price and easy to recycle, the reaction temperature is moderate, the production and control are easy; the raw material transformation rate is high; the target product selectivity is high, the yield is up to 91%, and the application prospect is wide. The formula (1) is shown in the description.
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Paragraph 0031; 0032; 0033; 0034; 0035; 0036; 0037-0042
(2017/09/01)
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- Copper-mediated ortho-nitration of (hetero)arenecarboxylates
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Various (hetero)arenecarboxylic acids were converted to the corresponding Daugulis amides and nitrated selectively in the ortho-position in the presence of [CuNO3(PPh3)2] and AgNO2 at 50 °C. A microwave-assisted saponification allows regenerating the carboxylate group within minutes, which may then be removed tracelessly by protodecarboxylation, or substituted by aryl- or alkoxy-groups via decarboxylative cross-coupling.
- Katayev, Dmitry,Pfister, Kai F.,Wendling, Timo,Goossen, Lukas J.
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p. 9902 - 9905
(2014/08/18)
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- Negishi-type coupling of bromoarenes with dimethylzinc
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Treatment of bromoarenes with dimethylzinc in the presence of a palladium catalyst provides a high-yielding route to methylarenes. The process accommodates a wide range of aromatic substituents and, in the majority of cases, is free of side reactions.
- Herbert, John M.
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p. 817 - 819
(2007/10/03)
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- Palladium-Catalyzed Hydroxycarbonylation of Aryl and Vinyl Halides or Triflates by Acetic Anhydride and Formate Anions ?
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(Equation presented) The palladium-catalyzed reaction of aryl and vinyl halides or triflates in the presence of acetic anhydride and lithium formate as a condensed source of carbon monoxide provides an efficient simple route to the synthesis of the corresponding carboxylic acids. The reaction proceeds very smoothly under mild conditions and tolerates a wide range of functional groups, including ether, ketone, ester, and nitro groups. The presence of ortho substituents does not hamper the reaction. Labeled carbonyl products can be easily prepared by using H13COONa.
- Cacchi, Sandro,Fabrizi, Giancarlo,Goggiamani, Antonella
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p. 4269 - 4272
(2007/10/03)
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- Discovery of novel phosphonic acid derivatives as new chemical leads for inhibitors of TNF-α production
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2-(Acylamino)benzylphosphonic acid 6 derived from an artificial substrate of sphingomyelinase was found to show inhibitory activity of TNF-α production. Structural optimization was started with the chemical modification of 6. The discovery of another chem
- Matsui, Toshiaki,Takahashi, Shinya,Matsunaga, Naoki,Nakamura, Kazunori,Omawari, Nagashige,Sakai, Masaru,Kamoshima, Wataru,Terai, Kouichiro,Ohno, Hiroyuki,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
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p. 3807 - 3815
(2007/10/03)
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- FUSED HETEROCYCLIC COMPOUNDS, HAVING ANGIOTENSIN II ANTAGONISTIC ACTIVITY
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Fused heterocyclic compounds of the formula (I): STR1 wherein R. sup.1 is an optionally substituted hydrocarbon residue which may be attached through a hetero atom; R 2 is a group capable of forming an anion or a group convertible thereinto; R 3 is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hetero atom; X is a direct bond or a spacer having an atomic length of two or less between the R 3 group and the ring W group; W is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hereto atom; a,c and d are independently selected from the group consisting of one or two optionally substituted carbon atoms and one or two optionally substituted hetero atoms; b and e are independently selected from the group consisting of one optionally substituted carbon atom and one optionally substituted nitrogen atom wherein one of b or e must be nitrogen; the dotted line is a bond to form one double bond; n is an integer of 1 or 2 and when a, which is an optionally substituted carbon atom, is taken together with R 1, the following group: STR2 may form a ring group; provided that when STR3 is a benzimidazole, thieno[3,4-d] imidazole, or thieno[2,3-d] imidazole ring, at least one of the group: STR4 and R 3 is an optionally substituted heterocyclic residue; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.
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- Herbicidally active enols
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Enols, their geometric isomers, tautomers and halogen addition products having the formula STR1 as defined herein and compositions containing these compounds exhibit herbicidal activity.
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