53498-62-7Relevant academic research and scientific papers
The formation of benzoxacin-3-ones: Via intramolecular Nicholas reactions and synthesis of 8-membered heliannuols
Green, James R.,St. Onge, Brent
supporting information, p. 7152 - 7155 (2021/08/30)
The γ-carbonyl cations generated from propargyl ether-Co2(CO)6 complexes undergo intramolecular Nicholas reactions to give dehydrobenzoxacin-3-one-Co2(CO)6 complexes in good yields. Reductive decomplexation and subsequent manipulation allows the synthesis of (±)-heliannuol K methyl ether and the formal syntheses of (±)-heliannuol K, (±)-heliannuol A, and (-)-heliannuol L.
Pd(II)-catalyzed ortho - Or meta-C-H olefination of phenol derivatives
Dai, Hui-Xiong,Li, Gang,Zhang, Xing-Guo,Stepan, Antonia F.,Yu, Jin-Quan
supporting information, p. 7567 - 7571 (2013/06/27)
A combination of weakly coordinating auxiliaries and ligand acceleration allows for the development of both ortho- and meta-selective C-H olefination of phenol derivatives. These reactions demonstrate the feasibility of directing C-H functionalizations when functional groups are distal to target C-H bonds. The meta-C-H functionalization of electron-rich phenol derivatives is unprecedented and orthogonal to previous electrophilic substitution of phenols in terms of regioselectivity. These methods are also applied to functionalize α-phenoxyacetic acids, a fibrate class of drug scaffolds.
Synthesis and preliminary antihyperlipidaemic activities evaluation of andrographolide derivatives
Wang, Bin,Tang, Chunlei,Han, Yaodan,Guo, Ruzhou,Qian, Hai,Huang, Wenlong
experimental part, p. 293 - 298 (2012/07/30)
Recent studies indicated that andrographolide was a potential antihyperlipidaemic therapeutic agent. In the paper, the synthesis of a series of andrographolide derivatives was described and their antihyperlipidaemic activities were evaluated in vivo. As compared with TG, TC, HDL-C and LDL-C concentrations, some of the derivatives exhibited better antihyperlipidaemic effects than positive control atromide. Therein, compound 6i, which was the most potent compound, could serve as a new lead for further development of antihyperlipidaemic agents.
Increasing selectivity of CC chemokine receptor 8 antagonists by engineering nondesolvation related interactions with the intended and off-target binding sites
Shamovsky, Igor,De Graaf, Chris,Alderin, Lisa,Bengtsson, Malena,Bladh, H?kan,B?rjesson, Lena,Connolly, Stephen,Dyke, Hazel J.,Van Den Heuvel, Marco,Johansson, Henrik,Josefsson, Bo-G?ran,Kristoffersson, Anna,Linnanen, Tero,Lisius, Annea,M?nnikk?, Roope,Nordén, Bo,Price, Steve,Ripa, Lena,Rognan, Didier,Rosendahl, Alexander,Skrinjar, Marco,Urbahns, Klaus
supporting information; experimental part, p. 7706 - 7723 (2010/07/04)
The metabolic stability and selectivity of a series of CCR8 antagonists against binding to the hERGion channel and cytochrome Cyp2D6 are studied by principal component analysis. It is demonstrated that an efficient way of increasing metabolic stability an
Development of a scalable synthesis of GSK183390A, a PPAR α/γ agonist
Oh, Lynette M.,Wang, Huan,Shilcrat, Susan C.,Hermann, Robert E.,Patience, Daniel B.,Spoors, P. Grant,Sisko, Joseph
, p. 1032 - 1042 (2012/12/30)
A scalable synthesis of GSK183390A, a PPAR α/γ agonist, is described. This synthesis is highlighted by (1) a regioselective formal 1,3-dipolar cycloaddition reaction between an enamine and a nitrile inline dipole to form a 1,3,5-trisubstmited pyrazole and (2) a regioselective amidomethylation of an o-cresol derivative using 2-chloro-JV- hydroxymethylacetamide.
INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
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Page/Page column 97, (2008/06/13)
The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatme
SUBSTITUTED PYRAZOLES AS PPAR AGONISTS
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Page/Page column 160, (2010/02/12)
A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof (I) wherein: p is O or 1; q is O or 1; R1 and R2 are independently H or C1-3 alkyl; R3 and R4 are independently H, C1-6 alkyl, -OC1-6 alkyl, halogen, OH, C2-6 alkenyl or CF3; R5 is H, C1-6 alkyl (optionally substituted by one or more halogens, -COphenyl, OC1-6 alkyl, phenyl morpholino or C2-6 alkenyl. R6 is C1-6 alkyl, halogen, -OCH2 phenyl, phenyl (optionally substituted by C1-3 alkiyl), morpholino, pyrrolidino, piperidino, thiophenyl, furanyl pyridinyl or -OC2-6 alkenyl. These compounds activate the alpha and gamma subtypes fo the hppar receptor and are useful e.g. in the treatment of diabetes, dyslipidemia or syndrome X.
