22833-69-8Relevant academic research and scientific papers
NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF DISEASES
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Paragraph 0448, (2020/12/11)
The present invention discloses compounds according to Formula (I), wherein R1a, R1b, R1c, R2a, W1, W2, X1, X2, X3, Y, and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
Total synthesis of diaportheone A
Tan, Mario A.,Züger, Patrik Peter,Roggo, Silvio
, p. 52 - 54 (2018/11/30)
Diaportheone A (1), a chromone natural product was previously isolated from the endophytic fungi Diaporthe sp. P 133. Its structure was established by spectroscopic methods, however, its absolute configuration remained undefined. This study dealt on the total synthesis of diaportheone A (1) utilizing the cyclization and in situ thermal syn-elimination of a β-ketosulfoxide. The C-1R absolute configuration of the natural product was established by X-ray crystallography of the synthetic diaportheone A (1) (>99% ee) and comparison with the optical rotation.
N,B-bidentate boryl ligand-supported iridium catalyst for efficient functional-group-directed C-H borylation
Wang, Guanghui,Liu, Li,Wang, Hong,Ding, You-Song,Zhou, Jing,Mao, Shuai,Li, Pengfei
supporting information, p. 91 - 94 (2017/05/16)
Convenient silylborane precursors for introducing N,B-bidentate boryl ligands onto transition metals were designed, prepared, and employed in ready formation of irdium(IIl) complexes via Si-B oxidative addition. A practical, efficient catalytic ortho-borylation reaction of arenes with a broad range of directing groups was developed using an in situ generated catalyst from the silylborane preligand 3c and [IrCl(COD)]2.
OPIOID RECEPTOR MODULATORS
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Page/Page column 142, (2016/06/14)
The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, 0, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alky
2-PYRIDYLOXY-3-ESTER-4-ETHER OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 53, (2015/06/25)
The present invention is directed to 2-pyridyloxy-3-ester-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prev
Circumambulatory movement of negative charge ("ring walk") during gas-phase dissociation of 2,3,4-trimethoxybenzoate anion
Herath, Kithsiri B.,Weisbecker, Carl S.,Singh, Sheo B.,Attygalle, Athula B.
, p. 4378 - 4389 (2014/06/09)
A dramatic "ortho effect" was observed during gas-phase dissociation of ortho-, meta-, and para-methoxybenzoate anions. Upon activation under mass spectrometric collisional activation conditions, anions generated from all three isomers undergo a CO2 loss. Of the m/z 107 ions generated in this way, only the 1-dehydro-2-methoxybenzene anion from the ortho isomer underwent an exclusive formaldehyde loss. A peak for a formaldehyde loss in the spectra of 2,4-, 2,5-, and 2,6-dimethoxybenzoates and the absence of an analogous peak from 3,4- and 3,5-dimethoxy derivatives confirmed that this is a diagnostically useful ortho-isomer-specific phenomenon. Moreover, the spectrum from 2,3-dimethoxybenzoic acid showed peaks for two consecutive formaldehyde losses. The 1-dehydro-2,3,4-trimethoxybenzene anion (m/z 167) generated from 2,3,4-trimethoxybenzoate in this way endures three consecutive eliminations of formaldehyde units. For this, the negative charge, initially located on position 1, circumambulates to position 2, then to position 3, and finally to position 4 to form the final phenyl anion. The proposed stepwise fragmentation pathway, which resembles the well-known E1cB-elimination mechanism, is supported by tandem mass spectrometric observations made with 2-[13C 2H3]methoxy-3-[13C]methoxy-4-methoxybenzoic acid, and ab initio calculations. In addition, the spectra of ions such as 1-dehydro-3,4-dimethoxybenzene anion show peaks for consecutive methyl radical losses, a feature that establishes the 1,2-relationship between the two methoxy groups.
BENZO-FUSED HETEROCYCLIC DERIVATIVES USEFUL AS AGONISTS OF GPR120
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Paragraph 0469, (2014/09/30)
The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
Stereoselective Formal Synthesis of (-)-Salicylihalamides A and B Via Prins Cyclisation
Yadav,Venkateswar Rao,Purushothama Rao,Sridhar Reddy,Prasad
scheme or table, p. 457 - 460 (2011/09/14)
A stereoselective and convergent formal approach to Salicylihalamide A and B is achieved through our recently developed strategy for the construction of polyketide precursors via Prins cyclisation. The approach mainly relies upon reductive opening of 1-iodomethyl cyclic ethers, Mitsunobu inversion and ring closing metathesis along with Prins cyclisation.
Synthesis and structural pattern recognition of 5-(2′-alkoxycarbonyl- substituted phenoxy)furfural derivatives
Chang, Chia-Lin
experimental part, p. 550 - 556 (2009/12/31)
The ethyl 5-(2′-alkoxycarbonyl-substituted phenoxy)furan-2- carboxylates (1C-13C) showed good antiplatelet aggregation,1) anti-allergic2) and anti-inflammatory activities.2) A series of 5-(2′-alkoxycarbonyl-substituted phenoxy)furfurals (1F-13F) were prepared for comparing the above activities. The objectives of this research are the synthesis and structural pattern recognition of compounds 1F-13F. The Silica Gel 60 column chromatography method was employed to separate and purify pure compounds 1F-13F by three solvent systems. For the structure elucidation of compounds 1F-13F, four spectroscopic methods were used: electron impact mass (EI-MS), UV-VIS, IR and NMR spectrometers. With the help of spectrometers, investigations can be performed on spectroscopic data. A simple methodology for recognizing structural patterns was carried out with the aid of statistical analysis designed to establish the classification model of the structural skeleton in this research. It was found that compounds 1C-13C and 1F-13F have similar chemical profiles and are clustered into one group. The pattern plots revealed valuable information and showed good correlation between compounds 1C-13C and 1F-13F. These findings correlate directly with the resulting spectroscopic data. These results with those obtained by EI-MS and NMR patterns give insight into a reliable pattern recognition for determining both 1C-13C and 1F-13F skeletons.
Synthesis of xanthones, thioxanthones, and acridones by the coupling of arynes and substituted benzoates
Zhao, Jian,Larock, Richard C.
, p. 583 - 588 (2007/10/03)
The reaction of silylaryl triflates, CsF, and ortho-heteroatom-substituted benzoates affords a general and efficient way to prepare biologically interesting xanthones, thioxanthones, and acridones. This chemistry presumably proceeds by a tandem intermolecular nucleophilic coupling of the benzoate with an aryne and a subsequent intramolecular electrophilic cyclization.
