1878-92-8Relevant academic research and scientific papers
Synthesis of N-Glycosyl-2-oxindoles by Pd-Catalyzed N-Arylation of 1-Amidosugars
Letribot, Boris,Redjdal, Wafa,Redjdal, Wafa,Benmerad, Belkacem,Le Bideau, Franck,Alami, Mouad,Messaoudi, Samir
supporting information, p. 4201 - 4206 (2020/06/04)
An efficient intramolecular Pd-catalyzed N-arylation of o-iodo-amidosugars for the synthesis of N-glycosylated oxindoles has been reported. The coupling reaction takes place in toluene and involves Pd(OAc)2/RuPhos catalytic systems in the presence of K2CO3. This versatile approach was extended successfully to the synthesis of other N-glycosylated heterocycles.
Finding new elicitors that induce resistance in rice to the white-backed planthopper Sogatella furcifera
He, Xingrui,Yu, Zhaonan,Jiang, Shaojie,Zhang, Peizhi,Shang, Zhicai,Lou, Yonggen,Wu, Jun
supporting information, p. 5601 - 5603 (2015/11/17)
Herein we report a new way to identify chemical elicitors that induce resistance in rice to herbivores. Using this method, by quantifying the induction of chemicals for GUS activity in a specific screening system that we established previously, 5 candidate elicitors were selected from the 29 designed and synthesized phenoxyalkanoic acid derivatives. Bioassays confirmed that these candidate elicitors could induce plant defense and then repel feeding of white-backed planthopper Sogatella furcifera.
Synthesis and biological evaluation of new quinoxaline derivatives of ICF01012 as melanoma-targeting probes
El Aissi, Radhia,Liu, Jianrong,Besse, Sophie,Canitrot, Damien,Chavignon, Olivier,Chezal, Jean-Michel,Miot-Noirault, Elisabeth,Moreau, Emmanuel
supporting information, p. 468 - 473 (2014/06/09)
The aim of this study was the synthesis and pharmacokinetic selection of a best melanin-targeting ligand for addressing anticancer agents to pigmented melanoma. Seven quinoxaline carboxamide derivatives were synthesized and radiolabeled with iodine-125. Biodistribution studies of compounds [ 125I]1a-g performed in melanoma-bearing mice tumor showed significant tumor uptake (range 2.43-5.68%ID/g) within 1 h after i.v. injection. Fast clearance of the radioactivity from the nontarget organs mainly via the urinary system gave high tumor-to-blood and tumor-to-muscle ratios. Given its favorable clearance and high tumor-melanoma uptake at 72 h, amide 1d was the most promising melanoma-targeting ligand in this series. Compound 1d will be used as building block for the design of new melanoma-selective drug delivery systems.
Copper-catalyzed one-pot synthesis of 2H-1,4-benzoxazin-3-(4H)-ones from 2-(o-haloaryloxy)acyl chlorides and primary amines
Hu, Qunxian,Xia, Ziming,Fan, Ling,Zheng, Jiening,Wang, Xiaoxia,Lv, Xin
experimental part, p. 129 - 142 (2012/05/04)
A facile and efficient Cu(I)-catalyzed one-pot synthesis of 2H-1,4-benzoxazin-3-(4H)-one derivatives has been developed. The condensation between 2-(o-haloaryloxy)acyl chlorides and primary amines followed by Cu(I)-catalyzed intramolecular C-N bond coupling afforded a variety of 2H-1,4-benzoxazin-3-(4H)-ones in good to excellent yields. Diversified substitutents on the 4-position could be conveniently introduced. ARKAT-USA, Inc.
COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES
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Page 25, (2010/02/08)
There are provided according to the invention, novel compounds of formula (I)wherein R, R, R, R, Rand Rare as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
Mild and reliable cleavage sequence for phenoxy acetates
Mirk, Daniela,Waldvogel, Siegfried R.
, p. 7911 - 7914 (2007/10/03)
A novel combination of reliable transformations like ester saponification and subsequent Curtius-rearrangement employing mild reaction conditions, offers the first synthetically interesting strategy for the removal of methoxycarbonylmethyl groups from phenolic oxygens. This methodology gives also access to labile iodosubstituted phenols. A novel combination of reliable transformations like ester saponification and subsequent Curtius-rearrangement employing mild reaction conditions, offers the first synthetically interesting strategy for the removal of methoxycarbonylmethyl groups from phenolic oxygens. This methodology gives also access to labile iodosubstituted phenols.
