249504-38-9Relevant academic research and scientific papers
Beta-amyloid protein targeting fluorescent probe, preparation and application of beta-amyloid protein targeting fluorescent probe in Alzheimer's disease
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Paragraph 0109; 0282-0286, (2021/06/09)
The invention discloses a beta-amyloid protein targeting fluorescent probe, preparation and application of the beta-amyloid protein targeting fluorescent probe in Alzheimer's disease. The structural formula of the fluorescent probe is as shown in formula I in the specification. The fluorescent probe disclosed by the invention is a compound taking 6-dimethylamino-1-methylquinoline as a parent structure, and the fluorescent probe has the advantages of long emission wavelength, large Stock shift, capability of specifically detecting beta amyloid protein, sensitivity to viscosity in tissue cells, and good response to the viscosity. After the fluorescent probe is combined with beta amyloid protein in the brain of a patient suffering from the Alzheimer's disease, a fluorescence signal is obviously enhanced, and the fluorescent probe can be used for detecting the beta amyloid protein and early diagnosing the Alzheimer's disease and has important guiding significance on development of diagnosis and treatment probes of the Alzheimer's disease.
Design, synthesis and evaluation of phenylthiazole and phenylthiophene pyrimidindiamine derivatives targeting the bacterial membrane
Chen, Yihua,Fan, Tingting,Guo, Weikai,Hu, Pan,Liu, Mingyao,Shao, Ting,Yi, Zhengfang,Zhou, Wenbo
, (2020/02/20)
As the continuous rise in the incidence of antibiotic resistance, it is urgent to develop novel chemical scaffolds with antibacterial activities to control the spread of resistance to conventional antibiotics. In this study, a series of phenylthiazole and
Novel 2-(5-aryl)thiophen-2-yl)benzimidazoles; design, synthesis and in vitro evaluation against cercarial phase of schistosoma mansoni
El Bialy, Serry A.,Mansour, Basem,Bayoumi, Waleed A.,Taman, Amira,Eissa, Hassan M.
, p. 1432 - 1438 (2020/10/06)
Background: Literature survey has pointed out that Benzimidazoles represent an interesting class of anthelmintics, of which several potent members were developed. Objective: Benzimidazoles hybridized with pharmacophoric moieties possessing anthelmintic ac
Preparation method of canagliflozin
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Paragraph 0014, (2019/02/27)
The invention relates to a synthesis method of canagliflozin. According to the synthesis method, 4-fluorophenylboronic acid is taken as an initial raw material to be coupled with 5-bromo-thiophene-2-formaldehyde to synthesize 5-(4-fluorophenyl)thiophene-2-formaldehyde, the 5-(4-fluorophenyl)thiophene-2-formaldehyde undergoes reduction and chlorination and then undergoes Friedel-Crafts alkylation reaction with 4-bromotoluene to synthesize 2-(2-methyl-5-bromobenzyl)-5-(4-fluorophenyl)thiophene, and the 2-(2-methyl-5-bromobenzyl)-5-(4-fluorophenyl)thiophene undergoes condensation, etherificationand methoxyl removal with 2,3,4,6-tetra-O-trimethylsilyl-D-gluconolactone to obtain the hypoglycemic drug canagliflozin. The preparation method has the following advantages: compared with the conventional preparation methods, the synthesis process takes the 4-fluorobenzeneboronic acid as an initial raw material, so that the raw material is cheap and easy to get, the process is easy to realize industrialization, the synthesis route is short and the operation is easy; in the synthesis process, bromine is not used or butyl lithium does not need to be used twice, so that the risk of the process can be reduced; in addition, the preparation method is capable of improving the yield of canagliflozin products to 70% or more.
Catalytic Deprotonative α-Formylation of Heteroarenes by an Amide Base Generated in Situ from Tetramethylammonium Fluoride and Tris(trimethylsilyl)amine
Shigeno, Masanori,Fujii, Yuki,Kajima, Akihisa,Nozawa-Kumada, Kanako,Kondo, Yoshinori
, p. 443 - 451 (2019/04/30)
Heteroarene formylations in DMF solution proceed in the presence of an amide base catalyst generated in situ from tetramethylammonium fluoride (TMAF) and tris(trimethylsilyl)amine (N(TMS)3). The reaction proceeds at room temperature and has an operationally simple procedure. Various heteroarenes, including benzothiophene, thiophene, benzothiazole, oxazole, and indole derivatives, can be formylated with high functional group tolerance.
A metal-free cascade reaction of β-halo-α,β-unsaturated aldehydes and 1,4-dithiane-2,5-diols: Synthesis of polycyclic 2-formylthiophenes
Goswami, Limi,Neog, Kashmiri,Sharma, Kumud,Gogoi, Pranjal
supporting information, p. 6470 - 6473 (2017/08/16)
A metal-free cascade reaction strategy has been developed for the synthesis of novel polycyclic 2-formylthiophenes from β-halo-α,β-unsaturated aldehydes and 1,4-dithiane-2,5-diols. A recyclable polymer supported organic base was used to perform the reaction process. This synthetic protocol was applied to synthesize several novel polycyclic thiophenes including steroidal D-ring annelated thiophene. Our synthetic strategy provides a high yield of thiophenes, avoids a tedious work-up procedure and minimizes the formation of waste.
Synthesis and evaluation of thiophene-based guanylhydrazones (iminoguanidines) efficient against panel of voriconazole-resistant fungal isolates
Ajda?i?, Vladimir,Senerovic, Lidija,Vrani?, Marija,Pekmezovic, Marina,Arsic-Arsnijevic, Valentina,Veselinovic, Aleksandar,Veselinovic, Jovana,?olaja, Bogdan A.,Nikodinovic-Runic, Jasmina,Opsenica, Igor M.
, p. 1277 - 1291 (2016/03/01)
A series of new thiophene-based guanylhydrazones (iminoguanidines) were synthesized in high yields using a straightforward two-step procedure. The antifungal activity of compounds was evaluated against a wide range of medicaly important fungal strains inc
Synthesis of 2-arylmethyl-5-aryl-thiophene
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Paragraph 0037; 0038, (2015/11/09)
The present invention provides a new synthetic process for the production of 2-arylmethyl-5-aryl-thiophene, an intermediate in the synthesis of C-aryl glycosides.
Facile synthesis of 1,2,3-triazole analogs of SGLT2 inhibitors by 'click chemistry'
Li, Lan-Tao,Zhou, Li-Fei,Li, Yan-Jun,Huang, Juan,Liu, Rui-Hua,Wang, Bin,Wang, Peng
supporting information; experimental part, p. 642 - 644 (2012/03/11)
Novel analogs of SGLT2 inhibitors containing the 1,2,3-triazole motif were designed and synthesized for urinary glucose excretion evaluation. The C-glucosides with triazole aglycone can be easily constructed by click chemistry. Most of the synthesized compounds increased urinary glucose excretion and demonstrated inhibition of glucose transport.
Synthesis of functionalized 2-arylthiophenes with triarylbismuths as atom-efficient multicoupling organometallic nucleophiles under palladium catalysis
Rao, Maddali L. N.,Banerjee, Debasis,Dhanorkar, Ritesh J.
supporting information; experimental part, p. 1324 - 1330 (2011/07/07)
Atom-efficient cross-coupling reactions of functionalized 2-bromo- and 2-iodothiophenes have been demonstrated using triarylbismuths as atom-efficient multicoupling organometallic nucleophiles under palladium-catalyzed conditions. These couplings with various functionalized triarylbismuths proceeded smoothly to afford the corresponding functionalized 2-arylthiophenes in high yields. Georg Thieme Verlag Stuttgart · New York.
