3624-90-6Relevant academic research and scientific papers
Group 4 metal complexes containing the salalen ligands: Synthesis, structural characterization and studies on the ROP of cyclic esters
Chakraborty, Debashis,Rajashekhar, Bijja,Mandal, Mrinmay,Ramkumar, Venkatachalam
, p. 111 - 121 (2018)
The synthesis of homoleptic salalen ligand supported group 4 complexes and their applications in the ring-opening polymerization (ROP) of ε-caprolactone (?-CL) and lactide (LA) are described. All these complexes of type M(L)2 (LH = (E)-N-(2-(3,
Synthesis of Structurally Diverse Benzotriazoles via Rapid Diazotization and Intramolecular Cyclization of 1,2-Aryldiamines
Faggyas, Réka J.,Sloan, Nikki L.,Buijs, Ned,Sutherland, Andrew
, p. 5344 - 5353 (2019/05/21)
An operationally simple method has been developed for the preparation of N-unsubstituted benzotriazoles by diazotization and intramolecular cyclization of a wide range of 1,2-aryldiamines under mild conditions, using a polymer-supported nitrite reagent and p-tosic acid. The functional group tolerance of this approach was further demonstrated with effective activation and cyclization of N-alkyl, -aryl, and -acyl ortho-aminoanilines leading to the synthesis of N1-substituted benzotriazoles. The synthetic utility of this one-pot heterocyclization process was exemplified with the preparation of a number of biologically and medicinally important benzotriazole scaffolds, including an α-amino acid analogue.
Fe-based metal-organic frameworks for the synthesis of N-arylsulfonamides via the reactions of sodium arylsulfinates or arylsulfonyl chlorides with nitroarenes in water
Li, Xinxin,Chen, Fei,Lu, Guo-Ping
, p. 4226 - 4230 (2018/10/26)
A newly developed chemoselective reaction of sodium arylsulfinates or arylsulfonyl chlorides with nitroarenes has been disclosed. The chemistry, in which non-toxic water and recyclable iron-based metal-organic frameworks are employed as the solvent and catalyst, respectively, provides an efficient approach for the generation of N-arylsulfonamides, which are widely present in biologically active compounds and drugs, rendering this methodology attractive to both synthetic and medicinal chemistry.
Amide type organic nitrogen ligand compound and synthesis method thereof
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Paragraph 0019; 0020; 0021, (2018/06/28)
The invention is claimed to protect an N-(2-(bis(2-hydroxyl-2-methyl propyl)amido)phenyl) amide type organic nitrogen ligand compound and a preparing method thereof. The method is simple and feasibleand is supplementation and development in the field of o
A novel serine racemase inhibitor suppresses neuronal over-activation in vivo
Mori, Hisashi,Wada, Ryogo,Takahara, Satoyuki,Horino, Yoshikazu,Izumi, Hironori,Ishimoto, Tetsuya,Yoshida, Tomoyuki,Mizuguchi, Mineyuki,Obita, Takayuki,Gouda, Hiroaki,Hirono, Shuichi,Toyooka, Naoki
, p. 3736 - 3745 (2017/06/13)
Serine racemase (SRR) is an enzyme that produces D-serine from L-serine. D-Serine acts as an endogenous coagonist of NMDA-type glutamate receptors (NMDARs), which regulate many physiological functions. Over-activation of NMDARs induces excitotoxicity, which is observed in many neurodegenerative disorders and epilepsy states. In our previous works on the generation of SRR gene knockout (Srr-KO) mice and its protective effects against NMDA- and Aβ peptide-induced neurodegeneration, we hypothesized that the regulation of NMDARs’ over-activation by inhibition of SRR activity is one such therapeutic strategy to combat these disease states. In the previous study, we performed in silico screening to identify four compounds with inhibitory activities against recombinant SRR. Here, we synthesized 21 derivatives of candidate 1, one of four hit compounds, and performed screening by in vitro evaluations. The derivative 13J showed a significantly lower IC50 value in vitro, and suppressed neuronal over-activation in vivo.
BENZENE SULFONAMIDE-BASED INHIBITORS OF SPHINGOSINE KINASE
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Paragraph 00137, (2016/03/13)
A novel class of sphingosine kinase (SK) inhibitor compounds are disclosed which are useful in the treatment of cancer and other proliferative cell conditions. The compounds are benzene sulfonamides with a chemical structure according to formula (I).
SERINE RACEMASE INHIBITOR
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Paragraph 0186 - 0190, (2014/12/12)
A novel serine racemase inhibitor exhibits sufficient activity and specificity. The serine racemase inhibitor includes one or more compounds selected from compounds respectively represented by the following general formulas [MM_1], [DR_1], [DR'_1], [LW_1], and [ED_1] as an active ingredient.
A one-pot synthetic strategy for construction of the dibenzodiazepine skeleton via a transition metal-free process
Fang, Shuai,Niu, Xiaoyi,Zhang, Zeyuan,Sun, Yan,Si, Xiaomeng,Shan, Cuicui,Wei, Lei,Xu, Aiqing,Feng, Lei,Ma, Chen
, p. 6895 - 6900 (2014/09/30)
A one-pot transition metal-free methodology for constructing pharmacologically active dibenzodiazepine derivatives was developed. Fluoro-, bromo- and nitro-substituted aryl aldehydes were applied to this reaction efficiently. This journal is the Partner Organisations 2014.
Palladium-catalyzed intramolecular sulfonamidation/oxidation of imines: Access to multifunctional benzimidazoles
Fu, Shaomin,Jiang, Huanfeng,Deng, Yuanfu,Zeng, Wei
experimental part, p. 2795 - 2804 (2011/12/01)
O-Sulfonamidophenylimines undergo intramolecular sulfonamidation/oxidation to produce 1,2-disubstituted benzimidazoles upon treatment with palladium(II) chloride/(diacetoxyiodo)benzene and potassium carbonate at room temperature. The substituent scope at
Highly enantioselective aldol reactions using N-arylprolinamides with enhanced acidity and double H-bonding potential
Saha, Satyajit,Moorthy, Jarugu Narasimha
supporting information; experimental part, p. 912 - 916 (2010/05/03)
We have designed and synthesized N-arylprolinamides 7-10 with a potential to involve in the binding of electrophilic aldehydes via two N-H?O hydrogen bonds for application in organocatalytic aldol reactions. The catalyst 10 is shown to afford aldol produc
