6725-44-6Relevant academic research and scientific papers
CHIMERIC COMPOUNDS AND METHODS OF MANAGING NEUROLOGICAL DISORDERS OR CONDITIONS
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Page/Page column 41, (2020/09/12)
This disclosure relates to chimeric compounds and methods for managing neurological conditions. In certain embodiments, the compound comprises a chemical structure of a monoamine reuptake inhibitor conjugated to a chemical structure of a histone deacetyla
Copper-Catalyzed and Indium-Mediated Methoxycarbonylation of Unactivated Alkyl Iodides with Balloon CO
Chen, Yanchi,Su, Lei,Gong, Hegui
supporting information, p. 4689 - 4693 (2019/06/27)
This work emphasizes the synthesis of alkyl esters via Cu-catalyzed and In-mediated alkoxycarbonylation of unactivated alkyl iodides in the presence of In or InI. The reactions were suitable for the preparation of primary, secondary, and even tertiary alkyl esters, representing an exceptionally rare example for the creation of quaternary carbon centers upon formation of esters. The preliminary mechanistic studies indicated that alkyl radicals were involved, and Cu/In/CO played a cooperative role in the carbonylation event.
Palladium-Catalyzed Asymmetric Allylic Alkylation of 4-Substituted Isoxazolidin-5-ones: Straightforward Access to β2,2-Amino Acids
Nascimento de Oliveira, Marllon,Arseniyadis, Stellios,Cossy, Janine
supporting information, p. 4810 - 4814 (2018/03/21)
We report here an unprecedented and highly enantioselective palladium-catalyzed allylic alkylation applied to 4-substituted isoxazolidin-5-ones. Ultimately, the process provides a straightforward access to β2,2-amino acids bearing an all-carbon quaternary stereogenic center in great yields and a high degree of enantioselectivity.
Synergistic Catalysis for the Umpolung Trifluoromethylthiolation of Tertiary Ethers
Xu, Wentao,Ma, Junyang,Yuan, Xiang-Ai,Dai, Jie,Xie, Jin,Zhu, Chengjian
supporting information, p. 10357 - 10361 (2018/08/06)
The first transition-metal-free, site-specific umpolung trifluoromethylthiolation of tertiary alkyl ethers has been developed, achieving the challenging tertiary C(sp3)–SCF3 coupling under redox-neutral conditions. The synergism of organophotocatalyst 4CzIPN and BINOL-based phosphorothiols can site-selectively cleave tertiary sp3 C(sp3)–O ether bonds in complex molecules initiated by a polarity-matching hydrogen-atom-transfer (HAT) event. The incorporation of several competing benzylic and methine C(sp3)?H bonds in alkyl ethers has little influence on the regioselectivity. Selective difluoromethylthiolation of C?O bonds has also been achieved. This represents not only an important step forward in trifluoromethylthiolation but also a promising means for site-selective C?O bond functionalization of unsymmetrical tertiary alkyl ethers.
Comparison of Phenylacetates with Benzoates and Phenylpropanoates as Antifeedants for the Pine Weevil, Hylobius abietis
Unelius, C. Rikard,Bohman, Bj?rn,Nordlander, G?ran
, p. 11797 - 11805 (2018/11/21)
This study concludes an extensive investigation of antifeedants for the pine weevil, Hylobius abietis (Coleoptera: Curculionidae), an economically important pest of planted conifer seedlings. Building on the previously reported antifeedant effects of benzoates and phenylpropanoids (aromatic compounds with one- or three-carbon-atom substituents on the benzene ring), we here report the antifeedant effects of compounds with two-carbon-atom side chains (i.e., phenylacetates). We also present new results; the best antifeedants from the benzoate class were tested at 10-fold lower concentrations in order to find the optimal antifeedants. Generally, for all three compound classes, efficient antifeedants were found to have one or two methyl, chloro, or methoxy substituents on the aromatic ring. For monosubstituted phenylpropanoids, the substituent preferably should be in the para-position. In the search for synergistic antifeedant effects among the three compound classes, combinations of compounds from the three classes were tested in binary and ternary mixtures.
Site-Selective Cross-Coupling of Remote Chlorides Enabled by Electrostatically Directed Palladium Catalysis
Golding, William A.,Pearce-Higgins, Robert,Phipps, Robert J.
supporting information, p. 13570 - 13574 (2018/10/20)
Control of site-selectivity in chemical reactions that occur remote from existing functionality remains a major challenge in synthetic chemistry. We describe a strategy that enables three of the most commonly used cross-coupling processes to occur with high site-selectivity on dichloroarenes that bear acidic functional groups. We have achieved this by repurposing an established sulfonylated phosphine ligand to exploit its inherent bifunctionality. Mechanistic studies suggest that the sulfonate group engages in attractive electrostatic interactions with the cation associated with the deprotonated substrate, guiding cross-coupling to the chloride at the arene meta position. This counterintuitive combination of anionic ligand and anionic substrate demonstrates an alternative design principle when considering the application of noncovalent interactions to direct catalysis.
USE OF AMITIFADINE, (+)-1-(3,4-DICHLOROPHENYL)-3-AZABICYCLO[3.1.0]HEXANE IN METHODS AND COMPOSITIONS WITH ENHANCED EFFICACY AND REDUCED METABOLIC SIDE EFFECTS AND TOXICITY FOR TREATMENT OF DEPRESSION AND OTHER CENTRAL NERVOUS SYSTEM DISORDERS AND CONDITIO
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Paragraph 0173, (2016/12/22)
The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable active salts, polymorphs, glycosylated derivatives, metabolites, solvates, hydrates, and/or prodrugs of (+)-1-(3,4-dichlorophenyl)-3-azab
Synthesis, Enzyme Inhibition, and Molecular Docking Studies of Hydrazones from Dichlorophenylacetic Acids
Abid, Obaid-Ur-Rahman,Ayaz, Muhammad,Rehman, Wajid,Mehdi, Kamran,Ali, Arif,Wadood, Abdul,Rahim, Fazal,Sultan, Aneesa,Ghufran, Mehreen,Mir, Sadullah,Qureshi, Muhammad Tauseef
, p. 1015 - 1021 (2016/12/22)
A series of hydrazones 5a–i were synthesized by the condensation of hydrazides derived from dichlorophenylacetic acids with different aromatic aldehydes and ketones. Their structures were confirmed by spectroscopic data and elemental analysis. Hydrazones
Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
Rahim, Fazal,Malik, Fazal,Ullah, Hayat,Wadood, Abdul,Khan, Fahad,Javid, Muhammad Tariq,Taha, Muhammad,Rehman, Wajid,Ur Rehman, Ashfaq,Khan, Khalid Mohammed
, p. 42 - 48 (2015/05/13)
Isatin base Schiff bases (1-20) were synthesized, characterized by 1H NMR and EI/MS and evaluated for α-glucosidase inhibitory potential. Out of these twenty (20) compounds only six analogs showed potent α-glucosidase inhibitory potential with IC50 value ranging in between 2.2 ± 0.25 and 83.5 ± 1.0 μM when compared with the standard acarbose (IC50 = 840 ± 1.73 μM). Among the series compound 2 having IC50 value (18.3 ± 0.56 μM), 9 (83.5 ± 1.0 μM), 11 (3.3 ± 0.25 μM), 12 (2.2 ± 0.25 μM), 14 (11.8 ± 0.15 μM), and 20 (3.0 ± 0.15 μM) showed excellent inhibitory potential many fold better than the standard acarbose. The binding interactions of these active analogs were confirmed through molecular docking.
Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students
Park, Jung-Eun,Song, Chiman,Choi, Keehyun,Sim, Taebo,Moon, Bongjin,Roh, Eun Joo
supporting information, p. 5515 - 5518 (2013/10/01)
A series of 3,4-diarylpyrrolidin-2-one was designed, prepared and evaluated as triple reuptake inhibitors for antidepressant. Most compounds exhibited comparable in vitro efficacy as norepinephrine and dopamine transporter reuptake inhibitors. Especially, 2i showed better potency than GBR-12909 (IC 50 = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM-85.6 nM) for three transporters.
