6274-54-0Relevant academic research and scientific papers
Method for synthesizing aryl alkyl sulfone compound by promoting oxidation of aryl alkyl thioether compound through visible light
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Paragraph 0049-0052; 0057-0060; 0068-0071, (2021/02/13)
The invention discloses a method for synthesizing an aryl alkyl sulfone compound by promoting oxidation of an aryl alkyl thioether compound through visible light. The method comprises the following steps of: performing one-pot reaction on an aryl alkyl thioether compound and sodium trifluoromethanesulfinate in a diethylene glycol dibutyl ether solution system under the conditions of oxygen-containing atmosphere and 385-390 nm purple light irradiation to generate the aryl alkyl sulfone compound. The method has the advantages of mild conditions, simple operation, environmental protection, easilyavailable raw materials, excellent compatibility of substrate functional groups, high reaction yield and the like.
Room Temperature Carbonylation of (Hetero) Aryl Pentafluorobenzenesulfonates and Triflates using Palladium-Cobalt Bimetallic Catalyst: Dual Role of Cobalt Carbonyl
Joseph, Jayan T.,Sajith, Ayyiliath M.,Ningegowda, Revanna C.,Shashikanth, Sheena
supporting information, p. 419 - 425 (2017/02/10)
An efficient method for the carbonylation of (hetero) aryl pentafluorobenzenesulfonates and triflates under exceptionally mild conditions using palladium/dicobalt octacarbonyl [Pd/Co2(CO)8] has been developed. Besides acting as carbon monoxide (CO) source, Co2(CO)8enhances the reaction rate by accelerating the CO insertion through an in situ generated bimetallic palladium cobalt tetracarbonyl [Pd-Co(CO)4] complex. Under the optimized reaction condition, carbonylation of a wide range of activated and deactivated, as well as sterically hindered and heteroaromatic, substrates proceeded efficiently at room temperature. The high chemoselectivity and improved synthesis of biologically relevant Isoguvacine and Lazabemide intermediates highlights its scope as a valuable synthetic method. The generality of this protocol was further extended to other electrophiles (bromides, chlorides and tosylates). (Figure presented.).
Synthesis of novel benzohydrazides bearing 4-[3-methyl-4-(methylsulfonyl)pyridin-2-yl] moiety as potential antibacterial agents
Saidugari, Swamy,Rao, V. Lakshmana,Vidya,Ram,Balram
, p. 639 - 643 (2016/01/20)
This work reports the synthesis and antibacterial activity of novel hydrazone derivatives 8a-k bearing 4-[3-methyl-4-(methylsulfonyl)pyridin- 2-yl] moiety. Spectroscopic techniques like 1H NMR, mass and IR tools was utilized for the characterization of these hydrazone derivatives. The synthesized hydrazone derivatives were tested against a set of bacterial strains, namely, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus pyogenes by paper disc diffusion method. Compounds 8b, 8d, 8e, 8f, 8h, 8i showed good antibacterial activity against the test organisms.
Synthesis, characterization and antimicrobial evaluation of novel (E)-N′-(4-(1-((3,4-dimethoxypyridin-2-yl)methyl)-1H-1,2,3-triazol-4-yl)benzylidene)benzohydrazide derivatives
Saidugari, Swamy,Vadali, Lakshmana Rao,Vidya,Ram
, p. 2155 - 2161 (2016/10/24)
The synthesis of novel 1,2,3-triazole-hydrazone derivatives embedded with 3,4-dimethoxy pyridine ring nucleus is described. These derivatives were prepared utilizing, 2-(chloromethyl)-3,4-dimethoxypyridine 1, 4-ethynylbenzaldehye 5 and various benzohydrazides7a-7j. The structures of the newly synthesized 1,2,3-triazole-hydrazones 8a-j was established on the basis of the spectroscopic techniques like 1H NMR, mass and IR data. They were evaluated against a panel of bacterial and fungal pathogens such as Staphylococcus. pyogens, Staphylococcus. Aureus (Gram positive bacteria), Escherichia.coli, Pseudomonas. aeruginosa (Gram negative bacteria) and Aspergillus niger and Candida albicans (Fungal stains). Compounds 8b, 8c, 8d, 8e and 8f with R = 4-OH, 4-OMe, 4-SO2Me, 3,45,-OMe and 3-NO2 respectively showed moderate antibacterial activity while compounds 8b, 8d, 8i and 8j with R = 4-OH, 4-SO2Me, 3,5-dichloro and 2,5-difluoro substitution exhibited very good fungal activity.
Synthesis and antibacterial activity of some new quinaxaline-benzohydrazides
Haripriya,Laxminarayana,Thirumala Chary
, p. 207 - 212 (2017/01/18)
Quinoxalines have been found to exhibit various biological activities such as antibacterial, antifungal, anti-tubercular, anxiolytic, anticancer, antioxidant, anti-inflammatory, anti-HIV, antihelmintic and anticonvulsant. The present study aims towards synthesis, characterization and determination of antimicrobial susceptibility testing of various novel quinoxaline derivatives. The quinoxaline-benzohydrazides 6a-m have been obtained by the condensation of quinoxaline-2-carboxaldehyde 4 with various benzohydrazides 5a-m in ethanol at reflux temperature. All the newly synthesized quinoxaline-benzohydrazide derivatives have been characterized by 1H NMR, IR and mass spectroscopic analysis. The synthesized quinoxaline-benzohydrazides 6a-m have been screened for antibacterial activity. Most of the compounds show significant antibacterial activity.
Synthesis and antimicrobial activity of new imidazole-hydrazone derivatives
Prasanna, V. Laxmi,Narender
, p. 3605 - 3608 (2015/12/24)
Hydrazones demonstrated significant antimicrobial activity, antitubercular activity and antitumoral activity in medicinal areas. The imidazole nucleus is well known to play an important role in living organisms since it is incorporated into the histidine molecule and many other important biological, pharmacological and therapeutic activities. Condensation of 4-phenyl-1H-imidazole-2-carbaldehyde (3) with various selected benzohydrazides (4a-m) resulted in imidazole-hydrazone derivatives (5a-m). They were evaluated for antibacterial and antifungal activity against A. Niger, C. albicans (fungal strains), E. coli and P. aeruginosa (Gram-negative bacteria), S. aureus and S. pyogenes (Gram-positive bacteria) using griseofluvin (for fungi) and ciprofloxacin (for bacteria) as the standard drugs. In general, it is observed that most of the compounds were found to be potent against both the bacterial and fungal strains.
Selective androgen receptor modulators
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Page/Page column 57-58, (2009/10/18)
This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.
Correlation pKa - activitee catalitique des thiols dans la reeaction d'hydrolyse de l'aceetate de p-nitropheenyle
Brembilla, Alain,Roizard, Denis,Schoenleber, Jacqueline,Lochon, Pierre
, p. 2330 - 2336 (2007/10/02)
The kinetic study of the hydrolysis of p-nitrophenylacetate in the presence of primary thiols indicates the thiolate anion as the sole catalytic species.Comparison of the true second order constants (kRS-) reveals that purely aliphatic primary thiols behave differently from aromatic α-substituted primary thiols.In the latter group a correlation can be established between the true second order rate constants and the pKSH values by means of the Broensted equation log kRS- = βpKSH + C, with β equal to 0.40 and C equal to -0.85.
