- Visible Light-Driven Carboxylation of Olefins by Using 2D Metal-Free Covalent Organic Framework as Intrinsic Photocatalyst: A Sustainable Approach for CO2 Utilization
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Photocatalytic metal-free carboxylation of olefins offers an environment-friendly approach for resolving the increasing energy issue as well as mitigating the dilemma caused by the greenhouse effect. Carboxylation of styrene and its derivatives by photocatalytic CO2 reduction reaction shows great potential for sustainable utilization of greenhouse gas CO2 into valuable chemicals. Herein, we have constructed a highly crystalline and thermally stable 2D porous covalent organic framework (COF) having very low band-gap energy, 1.8 eV and it shows efficient photocatalytic activity towards the carboxylation of aryl-alkenes in good yields in presence of p-terphenyl as a co-catalyst at ambient temperature under visible light irradiation and 1 atmospheric CO2 pressure which facilitates to overcome the current transition metal catalyzed approaches. In addition, TR-OT COF is a proficient and highly selective catalyst with outstanding recyclability. This suggests that this COF material is a novel photocatalyst for CO2 reduction towards α, β-carboxylation of styrene and its derivatives under 20 W light-emitting diode (LED) light.
- Das, Anjan,Ghosh, Swarbhanu,Manirul Islam, Sk.,Sarkar, Priyanka
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- Preparation method of alminoprofen intermediate
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The invention discloses a preparation method of an alminoprofen intermediate, belongs to the field of organic chemical synthesis, and provides a new technical route for improving the defects of synthetic reaction of ethyl 2-(4-amino-phenyl)propionate: 1) taking p-fluoronitrobenzene and diethyl methylmalonate as raw materials, adding alkali, conducting heating, finishing the reaction, conducting cooling, conducting hydrolyzing with alkali, after the reaction is finished, conducting layering, conducting washing with water, extracting impurities, adjusting the pH value, extracting a product, and conducting concentrating to obtain AMLF02; 2) heating AMLF02 in a solvent to 55-75 DEG C, and dropwise adding thionyl chloride for esterification reaction, conducting cooling, adjusting the pH, directly adding a catalyst for reduction at the temperature of 70-80 DEG C, after the reaction is finished, conducting filtering with the aid of diatomite, neutralizing the filtrate to 7-8, conducting concentrating to remove ethanol, extracting a water phase with methylbenzene, and conducting concentrating to obtain AMLF04. The method has the beneficial effects that the problem of slow filtration is solved, extraction is omitted, time is saved, and cost is saved; direct layering is performed after reaction, the amount of hydrochloric acid is reduced, and the treatment difficulty of three wastes is reduced; and safe hydrazine hydrate replaces active nickel.
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Paragraph 0048-0051; 0055-0058
(2021/07/21)
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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Paragraph 0625; 0628; 0629
(2016/09/26)
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- Palladium-catalyzed decarboxylative coupling of potassium nitrophenyl acetates with aryl halides
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A palladium-catalyzed decarboxylative cross-coupling of potassium 2- and 4-nitrophenyl acetates with aryl chlorides and bromides has been developed. Because the nitro group can be readily converted to many other functional groups, the new reaction provides a useful method for the preparation of diverse 1,1-diaryl methanes and their derivatives.
- Shang, Rui,Huang, Zheng,Chu, Ling,Fu, Yao,Liu, Lei
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supporting information; experimental part
p. 4240 - 4243
(2011/10/09)
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- Direct amino acid-catalyzed cascade reductive alkylation of arylacetonitriles: High-yielding synthesis of ibuprofen analogs
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A novel approach for a one-pot, three-component reductive alkylation (TCRA) reaction of arylacetonitriles-containing electron-withdrawing groups with aldehydes/ketones and 1,4-dihydropyridine via iminium-catalysis has been developed. Many TCRA reaction products have direct applications in agricultural and pharmaceutical chemistry.
- Ramachary, Dhevalapally B.,Shiva Prasad
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scheme or table
p. 5246 - 5251
(2010/11/03)
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- Vanilloid Receptor Ligands, Pharmaceutical Compositions Containing Them, Process for Making Them, and Use Thereof for Treating Pain and Other Conditions
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Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.
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Page/Page column 62; 63; 64; 65
(2009/07/03)
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- Experiments on the Chaperon effect in the nitration of aromatics
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A nitro group may be effectively delivered to the ortho position of alkylbenzenes, provided that a suitable chaperon function is located in α- position and a dilute of HNO3 in CH2Cl2 is used. The carbonyl function of an aldehyde or ketone is the best choice, but a carboxyl, alkoxycarbonyl, and amide groups all work well. The ether function showed a less pronounced ortho orientation effect, whereas the hydroxyl group was too prone to oxidation. Side reactions were minimal under the conditions employed. A para chaperon effect was seemingly at work in the CH2Cl2 nitration of benzenepropanenitrile. All the results were compared with the corresponding classical nitration in H2SO4.
- Strazzolini, Paolo,Giumanini, Angelo G.,Runcio, Antonio,Scuccato, Massimo
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p. 952 - 958
(2007/10/03)
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- Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 1. Tropic and 2-phenylpropionic acid esters
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Previous studies have shown that (R)-(+)-hyoscyamine has analgesic activity as a consequence of increased ACh release following antagonism of central muscarinic autoreceptors. Since the enhancement of central cholinergic transmission could be beneficial for cognitive disorders, we manipulated (R)-(+)-hyoscyamine, synthesizing several derivatives of tropic and 2-phenylpropionic acids, with the aim of obtaining drugs which are able to increase ACh release and consequently to show analgesic and nootropic activities. The results showed that several new compounds are indeed potent analgesics (with an analgesic efficacy comparable to that of morphine) and that the most potent one ((±)-19, PG9) also has remarkable cognition- enhancing properties. Our study confirmed that the mechanism of action involves ACh release even if it is still unclear whether only muscarinic autoreceptors or, also, heteroreceptors are involved.
- Gualtieri,Conti,Dei,Giovannoni,Nannucci,Romanelli,Scapecchi,Teodori,Fanfani,Ghelardini,Giotti,Bartolini
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p. 1704 - 1711
(2007/10/02)
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- Carbaphens: aprophen analogs that are binary antidotes for organophosphate poisoning
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Novel carbaphens are provided of the formula STR1 wherein R is OH, OCON(CH3)2 or OCONHCH3, and R' is H, OH or 2 OCON(CH3)2, stereoisomers thereof, pharmaceutically-acceptable salts thereof or mixtures thereof. Compositions comprise the carbaphens with pharmaceutically acceptable carriers, and they may further comprise other drugs as well. Methods of treating patients either prophylactically or therapeutically which suffer from organophosphate poisoning, coronary insufficiency, cerebral vasospasms, spastic cholitis and cholecystitis comprise the administration of the carbaphens of the invention.
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- Immunomodulating agent
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Phenylacetic acid derivatives of the formula: STR1 wherein R1 is hydrogen or STR2 wherein R5 is an alkyl group of 1-6 carbon atoms or an aryl group; R2 and R3 are independently hydrogen or an alkyl group of 1-4 carbon atoms; R4 is hydrogen or an alkyl group of 1-4 carbon atoms, have been found to possess immunomodulating activity.
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- α-Nitroarylation of Ketones and Esters: An Exceptionally Facile Synthesis of Indoles, 2-Indolinones, and Arylacetic Acids
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Silyl enol ethers and ketene silyl acetals add to aromatic nitro compounds in the presence of fluoride ion sources to give dihydroaromatic nitronates which are readily oxidized to α-nitroaryl carbonyl compounds by DDQ or Br2.These versatile intermediates are readily converted into indoles or 2-indolinones by reductive cyclization.Since halogen substituents on the aromatic ring are not displaced in the initial alkylation reaction, nucleophilic substitution of these groups, followed by functional group manipulations of the nitro group, permits easy access to indoles, 2-indolinones, and arylacetic acids with varied substitution patterns.
- RajanBabu, T. V.,Chenard, Bertrand L.,Petti, Michael A.
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p. 1704 - 1712
(2007/10/02)
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- Nucleophilic substitution process
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Nitroarylacetic acid esters are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base so that the ester undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their esters are useful intermediates for the synthesis of pharmaceuticals.
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- Nonsteroidal antiinflammatory agents. 2. [(Heteroarylamino)phenyl]alkanoic acids
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A series of [(heteroarylamino)phenyl]alkanoic acids pyridine, quinoline, or pyrimidine as the heteroaryl moiety was prepared as potential antiinflammatory agents. Among them, 2-[4-(2-pyridylamino)phenyl]propionic acid (14b) showed excellent antiinflammatory and analgesic activities with less tendency to cause gastric side effects. Structure-activity relationships are discussed.
- Hino,Nakamura,Nagai,Uno,Nishimura
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p. 222 - 226
(2007/10/02)
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- Process for the preparation of 2-(4'-nitrophenyl)-propionic acid
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The present invention concerns a process for the preparation of 2-(4'-nitrophenyl)-propionic acid of the formula (I): STR1 More particularly, this invention relates to a process for the preparation of 2-(4'-nitrophenyl)-propionic acid (I) starting from para-nitroethylbenzene (PNEB) by carboxylation in the presence of alkaline phenates (Na and K). The 2-(4'-nitrophenyl)-propionic acid (I) thus obtained finds a useful application as an intermediate for the preparation of chemical products. For instance, acid (I) may be hydrogenated catalytically until obtaining the corresponding amino-derivative which is then condensed with ortho-cyanobenzyl-bromides in order to give isoindoline (as described in Belgian Pat. No. 774985).
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