326902-40-3Relevant academic research and scientific papers
Synthesis, Biological Evaluation of ortho-Carboxamidostilbenes as Potential Inhibitors of Hyperglycemic Enzymes, and Molecular Docking Study
Abu Bakar, Mohamad Hafizi,Awang, Khalijah,Azmi, Mohamad Nurul,Che Omar, Mohammad Tasyriq,Mohamad, Norhadi,Phua, Yoong Hui,Supratman, Unang,Wahab, Habibah A.
, (2021/07/21)
A new series of ortho-carboxamidostilbenes derivatives were synthesized via Heck Coupling and screened for their α-amylase and α-glucosidase inhibitory potential. The results indicated that all the synthesized compounds showed a substantial α-glucosidase
Novel and efficient heterogeneous polymer supported copper catalyst for synthesis of 2-substituted Benzoxazoles from 2-Haloanilides
Saranya, Thachora Venu,Sruthi, Pambingal Rajan,Raj, Veena,Anas, Saithalavi
supporting information, (2021/02/27)
A novel polymer supported copper complex is prepared by the immobilization of copper iodide on chemically modified polyacrylonitrile and its application in heterogeneous catalysis is described. The catalyst was prepared by easy method via synthetic modification of Polyacrylonitrile (PAN) using ethylene diamine followed by the complexation with CuI. After characterization, this complex was explored as a green and efficient heterogeneous catalyst for the synthesis of 2-benzoxazoles from 2-haloanilides. The reaction was performed without adding additional ligand and the catalyst shows activity over a broad range of substrates with quantitative product yields. The catalyst was easily recovered by simple filtration and reused successfully for further cycle.
Facile synthesis of 2-benzoxazoles via CuI/2,2'-bipyridine catalyzed intramolecular C–O coupling of 2-haloanilides
Venu Saranya, Thachora,Rajan Sruthi, Pambingal,Anas, Saithalavi
supporting information, p. 297 - 307 (2019/01/18)
Development of newer methods for the synthesis of Benzoxazoles has of greater interest due to their wide range of biological activities and pharmaceutical importance. We herein report a facile and general method for the synthesis of 2-substituted Benzoxazoles via copper catalyzed intramolecular C–O cross-coupling of 2-haloanilides. A combination of CuI (5 mol%), 2,2'-bipyridine (10 mol%), Cs2CO3 (2 equiv.) in DMF solvent with 4 ? molecular sieves at 140 °C, illustrated the scope for tuning the reactivity of 2-haloanilides toward the selective formation of a series of 2-alkyl benzoxazole derivatives in moderate to good yields. This is the first systematic study using CuI/2,2'-Bipyridine as the catalytic system for the synthesis of 2-substituted Benzoxazoles. The outcome of the reaction was found to be significantly influenced by the aromatic and amide substituents of 2-haloanilides.
Photoredox-Induced Intramolecular 1,5-H Transfer Reaction of Aryl Iodides for the Synthesis of Spirocyclic γ-Lactams
Chen, Jian-Qiang,Chang, Rui,Lin, Jun-Bing,Luo, Yong-Chun,Xu, Peng-Fei
supporting information, p. 2395 - 2398 (2018/04/30)
This work develops a photocatalysis method for the synthesis of γ-spirolactams through a tandem intramolecular 1,5-HAT reaction-cyclization process. A variety of novel γ-spirolactams are prepared in good to excellent yields with this method. This transfor
Intramolecular 1,5-H transfer reaction of aryl iodides through visible-light photoredox catalysis: A concise method for the synthesis of natural product scaffolds
Chen, Jian-Qiang,Wei, Yun-Long,Xu, Guo-Qiang,Liang, Yong-Min,Xu, Peng-Fei
supporting information, p. 6455 - 6458 (2016/05/24)
The intramolecular 1,5-H transfer reaction of the aryl radicals generated from unactivated aryl iodides by photocatalysis is described. The features of this transformation are operational simplicity, excellent yields, mild reaction conditions, and good fu
Challenges associated with the synthesis of unusual o-carboxamido stilbenes by the Heck protocol: Intriguing substituent effects, their toxicological and chemopreventive implications
Kee, Chin Hui,Ariffin, Azhar,Awang, Khalijah,Takeya, Koichi,Morita, Hiroshi,Hussain, Salmaan Inayat,Chan, Kok Meng,Wood, Pauline J.,Threadgill, Michael D.,Lim, Chuan Gee,Ng, Seikweng,Weber, Jean Frederic F.,Thomas, Noel F.
experimental part, p. 5646 - 5660 (2011/02/18)
The syntheses of fourteen unusual o-carboxamido stilbenes by the Heck protocol revealed surprising complexity related to intriguing substituent effects with mechanistic implications. The unexpected cytotoxic and chemopreventive properties also seem to be substituent dependent. For example, although stilbene 15d (with a 4-methoxy substituent) showed cytotoxicity on HT29 colon cancer cells with an IC50 of 4.9 μM, the 3,4-dimethoxy derivative (15c) is inactive. It is interesting to observe that the 3,5-dimethoxy derivative (15e) showed remarkable chemopreventive activity in WRL-68 fetal hepatocytes, surpassing the gold standard, resveratrol. The resveratrol concentration needed to be 5 times higher than that of 15e to produce comparable elevation of NQO1.
Synthesis, structure, and chemoselective reactivity of N-(2-iodylphenyl) acylamides: Hypervalent iodine reagents bearing a pseudo-six-membered ring.scaffold
Ladziata, Uladzimir,Koposov, Alexey Y.,Lo, Ka Y.,Willging, Jeff,Nemykin, Victor N.,Zhdankin, Viktor V.
, p. 7127 - 7131 (2007/10/03)
A pseudo-benziodoxazine structure with intramolecular secondary I...O bonding, as shown by X-ray analysis, is seen in a series of N-(2-iodylphenyl) acylamides prepared from 2-iodoaniline (see scheme). These compounds contain a six-membered pseudocyclic scaffold about an iodine(v) center and are able to oxidize either alcohols or sulfides, with the reactivity depending largely on the substitution pattern on the amide group adjacent to the iodyl moiety. (Chemical Equation Presented).
SUBSTITUTED ANILINIC PIPERIDINES AS MCH SELECTIVE ANTAGONISTS
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Page column 179, (2010/02/06)
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
