103258-38-4Relevant academic research and scientific papers
Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors
Papillon, Julien P. N.,Adams, Christopher M.,Hu, Qi-Ying,Lou, Changgang,Singh, Alok K.,Zhang, Chun,Carvalho, Jose,Rajan, Srinivan,Amaral, Adam,Beil, Michael E.,Fu, Fumin,Gangl, Eric,Hu, Chii-Whei,Jeng, Arco Y.,LaSala, Daniel,Liang, Guiqing,Logman, Michael,Maniara, Wieslawa M.,Rigel, Dean F.,Smith, Sherri A.,Ksander, Gary M.
, p. 4749 - 4770 (2015/06/25)
CYP11B2, the aldosterone synthase, and CYP11B1, the cortisol synthase, are two highly homologous enzymes implicated in a range of cardiovascular and metabolic diseases. We have previously reported the discovery of LCI699, a dual CYP11B2 and CYP11B1 inhibi
Phthalide: A direct building-block towards P,O and P,N hemilabile ligands. Application in the palladium-catalysed Suzuki-Miyaura cross-coupling of aryl chlorides
McNulty, James,Keskar, Kunal
supporting information, p. 2404 - 2407 (2013/06/05)
The direct synthesis of new hemilabile ligands from the economical, readily available lactone phthalide is described. Pd-complexes of one such ligand were found highly effective in general Suzuki-Miyaura cross-coupling reactions, including deactivated and hindered aryl chlorides. The Royal Society of Chemistry 2013.
ORGANIC COMPOUNDS
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Page/Page column 58, (2008/06/13)
The present invention provides a compound of formula (I):said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.
Mapping and fitting the peripheral benzodiazepine receptor binding site by carboxamide derivatives. Comparison of different approaches to quantitative ligand-receptor interaction modeling
Anzini,Cappelli,Vomero,Seeber,Menziani,Langer,Hagen,Manzoni,Bourguignon
, p. 1134 - 1150 (2007/10/03)
The synthetic-computational approach to the study of the binding site of peripheral benzodiazepine receptor (PBR) ligands related to 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide (PK11195, 1) within their receptor (Cappelli et a
Sparteine-mediated enantioselective [2,3]-Wittig rearrangement of allyl ortho-substituted benzyl ethers and ortho-substituted benzyl prenyl ethers
Kawasaki, Takeshi,Kimachi, Tetsutaro
, p. 6847 - 6862 (2007/10/03)
The (-)-sparteine-mediated enantioselective [2,3]-Wittig rearrangement of N,N-dialkyl-o-allyloxymethylbenzamides and o-substituted benzyl prenyl ethers has been investigated. Enantiomeric excess up to 60% was observed as for the reaction with N,N-diethyl-o-allyloxymetylbenzamide. From the mechanistic investigations, it was suggested that the stereoinformation was introduced at the deprotonation step. Substoichiometric amount of (-)- sparteine (0.2 equiv.) did not decrease the enantioselectivity. Introduction of functional groups other than carbamoyl group did not enhance the enantioselectivity in this rearrangement.
Enantioselective [2,3]-Wittig rearrangement via sparteine-mediated lateral metalation of N,N-dialkyl-o-allyloxymethylbenzamides and o-substituted benzyl prenyl ethers
Kawasaki, Takeshi,Kimachi, Tetsutaro
, p. 1429 - 1431 (2007/10/03)
The (-)-sparteine-mediated enantioselective [2,3]-Wittig rearrangement of N,N-dialkyl-o-allyloxymethylbenzamides and o-substituted benzyl prenyl ethers has been investigated. With N,N-diethyl-o-allyloxymethylbenzamide, enantiomeric excess up to 60% was observed in pentane. These results suggest that the carbamoyl group can effectively assist the transfer of stereoinformation by coordinating with the (-)-sparteine-n-BuLi complex. Other functional groups (OMe, OCONR2, OMOM, F) were impotent to the enantiodifferentiation of this rearrangement.
Hydroxylation of carbanions with lithium teri-butyl peroxide acting as an oxenoid
Julia, Marc
, p. 15 - 24 (2007/10/03)
The lithium salt of terf-butyl hydroperoxide can convert alkyl, vinyl, aryl carbanions, acetylides and various enolates into the corresponding hydroxylated derivatives in good yields and under mild conditions. Eisevier.
Aluminium chloride mediated aminolysis of lactones: A general method for the preparation of ω-hydroxyalkylamides
Lesimple,Bigg
, p. 306 - 308 (2007/10/02)
Medium-ring lactones react cleanly with primary and secondary aliphatic or aromatic amines in the presence of aluminium chloride at room temperature to afford ω-hydroxyalkylamides in high yield.
α',α'-DISILYLATED TERTIARY BENZAMIDES AS DUAL ORTHO- AND α'-CARBANION SYNTHONS. AMIDE PETERSON OLEFINATION ROUTES TO N-BENZOYL ENAMINES, ISOQUINOLINES, AND DIBENZAZOCINES
Cuevas, J.-C.,Patil, P.,Snieckus, V.
, p. 5841 - 5844 (2007/10/02)
α',α'-Disilylated benzamides 2, prepared by LiTMP/TMSCl in situ trap procedure, constitute ortho- and α'-carbanion synthons which provide N-benzoyl enamines (5), isoquinolines (6), dibenzoazocines (9) by Peterson olefination, and pyrroles (11) by cycloaddition.The conversion of 2 into other useful functionality is described.
