699-91-2Relevant academic research and scientific papers
GaCl3-catalyzed ortho-ethynylation of phenols
Kobayashi, Katsumi,Arisawa, Mieko,Yamaguchi, Masahiko
, p. 8528 - 8529 (2002)
Phenols are ethynylated at the ortho position with silylated chloroethyne in the presence of a catalytic amount of GaCl3 and lithium phenoxide. The lithium salt is essential for the catalysis, and addition of 2,6-di(tert-butyl)-4-methylpyridine
Electrophotocatalytic C?H Heterofunctionalization of Arenes
Huang, He,Lambert, Tristan H.
supporting information, p. 11163 - 11167 (2021/04/19)
The electrophotocatalytic heterofunctionalization of arenes is described. Using 2,3-dichloro-5,6-dicyanoquinone (DDQ) under a mild electrochemical potential with visible-light irradiation, arenes undergo oxidant-free hydroxylation, alkoxylation, and amination with high chemoselectivity. In addition to batch reactions, an electrophotocatalytic recirculating flow process is demonstrated, enabling the conversion of benzene to phenol on a gram scale.
Efficient preparation method of 2'-hydroxyacetophenone compounds
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Paragraph 0029; 0030; 0032; 0033, (2019/05/08)
The invention discloses an efficient preparation method of 2'-hydroxyacetophenone compounds. The method comprises the following steps: substituted phenol and acetic anhydride in a molar ratio of 1:(1-1.1) is subjected to a reaction at 130-150 DEG C in the absent of a solvent, acetic acid substituted phenyl ester as shown in the formula is generated, and acetic acid and acetic acid substituted phenyl ester are separated by rectification; prepared acetic acid substituted phenyl ester is subjected to a transposition reaction under the action of a catalyst in an organic solvent at the temperatureof 50-120 DEG C, and 2'-hydroxyacetophenone compounds as shown in the formula are generated; filtering is performed to remove the catalyst after the reaction is finished, the solvent is removed by evaporation, and the 2'-hydroxyacetophenone compounds are prepared by rectification under vacuum, wherein the catalyst is phosphomolybdic acid, phosphotungstic acid, silicotungstic acid or a mixture of the acid. The preparation method has mild conditions and simple flow, and is environmentally friendly and suitable for industrial production, selectivity is high, and ortho-position selectivity is as high as 99.5%.
Iridium-Catalyzed C(sp3)?H Addition of Methyl Ethers across Intramolecular Carbon–Carbon Double Bonds Giving 2,3-Dihydrobenzofurans
Ohmura, Toshimichi,Kusaka, Satoshi,Torigoe, Takeru,Suginome, Michinori
supporting information, p. 4448 - 4453 (2019/09/16)
Intramolecular addition of an O-methyl C(sp3)?H bond across a carbon-carbon double bond occurs in the iridium-catalyzed reaction of methyl 2-(propen-2-yl)phenyl ethers. The Ir/(S)-DTBM-SEGPHOS catalyst promotes the reaction efficiently in toluene at 110–135 °C to afford 3,3-dimethyl-2,3-dihydrobenzofurans. Enantioselective C(sp3)?H addition is achieved in the reaction of methyl 2-(1-siloxyethenyl)phenyl ethers, affording enantioenriched 3-hydroxy-2,3-dihydrobenzofuran derivatives with up to 96% ee. (Figure presented.).
Ultrasound-assisted synthesis and antimicrobial activity of tetrazole-based pyrazole and pyrimidine derivatives
Dofe, Vidya S.,Sarkate, Aniket P.,Shaikh, Zarina M.,Gill, Charansingh H.
, p. 59 - 65 (2018/01/18)
New tetrazole-based pyrazole and pyrimidine derivatives were synthesized by an ultrasound irradiation method. All compounds were characterized by infrared spectroscopy (IR), 1H nuclear magnetic resonance (NMR), 13C NMR, mass spectrometry (MS) and elemental analysis and assessed in vitro for their efficacy as antimicrobial agents against four bacteria (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa) and two fungi (Candida albicans, Aspergillus Niger). Compounds 8a, 8e, 9a, 9b and 9e show potent activity against the tested strains compared to the reference drugs chloramphenicol and clotrimazole.
Synthesis, antimicrobial activity and anti-biofilm activity of novel tetrazole derivatives
Dofe, Vidya S.,Sarkate, Aniket P.,Kathwate, Santosh H.,Gill, Charansingh H.
, p. 325 - 330 (2017/08/18)
In the development of antimicrobial agents, we designed and synthesized novel tetrazole derivatives. The structures of compounds 6a-f and 7a-f were characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis. These compounds were tested for their antimicrobial activity against a series of strains Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa and for antifungal activity against the strains Candida albicans, Candida glabrata, and Candida tropicalis. Compounds 6e, 6f, 7a, and 7f exhibit potent antimicrobial activities compared to the reference drugs streptomycin and miconazole. Tetrazole derivatives 7a-f also inhibit biofilm formation and compound 7f exhibits best anti-biofilm activity with a biofilm inhibitory concentration (BIC) as low as 0.9 μm.
Effects of structural modifications on the metal binding, anti-amyloid activity, and cholinesterase inhibitory activity of chalcones
Fosso, Marina Y.,LeVine, Harry,Green, Keith D.,Tsodikov, Oleg V.,Garneau-Tsodikova, Sylvie
supporting information, p. 9418 - 9426 (2015/09/15)
As the number of individuals affected with Alzheimer's disease (AD) increases and the availability of drugs for AD treatment remains limited, the need to develop effective therapeutics for AD becomes more and more pressing. Strategies currently pursued include inhibiting acetylcholinesterase (AChE) and targeting amyloid-β (Aβ) peptides and metal-Aβ complexes. This work presents the design, synthesis, and biochemical evaluation of a series of chalcones, and assesses the relationship between their structures and their ability to bind metal ions and/or Aβ species, and inhibit AChE/BChE activity. Several chalcones were found to exhibit potent disaggregation of pre-formed N-biotinyl Aβ1-42 (bioAβ42) aggregates in vitro in the absence and presence of Cu2+/Zn2+, while others were effective at inhibiting the action of AChE.
Pyrazolopyrrolidine Derivatives and their Use in the Treatment of Disease
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Paragraph 0739; 0740, (2014/12/09)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
PYRAZOLOPYRROLIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 147, (2014/12/12)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
IMIDAZOPYRROLIDINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 104; 105, (2014/12/12)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
