915089-10-0Relevant academic research and scientific papers
The discovery of orally bioavailable tyrosine threonine kinase (TTK) inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as anticancer agents
Liu, Yong,Lang, Yunhui,Patel, Narendra Kumar,Ng, Grace,Laufer, Radoslaw,Li, Sze-Wan,Edwards, Louise,Forrest, Bryan,Sampson, Peter B.,Feher, Miklos,Ban, Fuqiang,Awrey, Donald E.,Beletskaya, Irina,Mao, Guodong,Hodgson, Richard,Plotnikova, Olga,Qiu, Wei,Chirgadze, Nickolay Y.,Mason, Jacqueline M.,Wei, Xin,Lin, Dan Chi-Chia,Che, Yi,Kiarash, Reza,Madeira, Brian,Fletcher, Graham C.,Mak, Tak W.,Bray, Mark R.,Pauls, Henry W.
supporting information, p. 3366 - 3392 (2015/05/05)
The acetamido and carboxamido substituted 3-(1H-indazol-3-yl)benzenesulfonamides are potent TTK inhibitors. However, they display modest ability to attenuate cancer cell growth; their physicochemical properties, and attendant pharmacokinetic parameters, a
2,2- and 2,6-diarylpiperidines by aryl migration within lithiated urea derivatives of tetrahydropyridines
Tait, Michael B.,Butterworth, Sam,Clayden, Jonathan
supporting information, p. 1236 - 1239 (2015/03/14)
2-Aryltetrahydropyridines formed by anionic cyclization or ring-closing metathesis were converted to their N′-aryl urea derivatives. Depending on the position of the unsaturation within the tetrahydropyridine ring, metalation by deprotonative lithiation or carbolithiation led to migration of the N′-aryl substituent to the 2- or 6-position via intramolecular nucleophilic attack of a benzylic organolithium on the aryl ring. The products are a range of 2,2-, 2,2,3-, and 2,6-polysubstituted piperidine derivatives. Related chemistry was observed in pyrroline homologues.
Cycloaddition of chiral tert -butanesulfinimines with trimethylenemethane
Procopiou, George,Lewis, William,Harbottle, Gareth,Stockman, Robert A.
supporting information, p. 2030 - 2033 (2013/06/05)
The cycloaddition of chiral tert-butanesulfinimines with trimethylenemethane is found to give facile access to methylene-pyrrolidines with good yields and diastereoselectivities. The full scope of the cycloaddition is explored, and a range of transformations of the formed methylenepyrrolidines to give a range of functionalized chiral pyrrolidines is presented.
Asymmetric synthesis of amines by the knochel-type MgCl2- enhanced addition of benzyl zinc reagents to N -tert -Butanesulfinyl aldimines
Buesking, Andrew W.,Baguley, Tyler D.,Ellman, Jonathan A.
supporting information; experimental part, p. 964 - 967 (2011/04/26)
The MgCl2-enhanced addition of benzyl zinc reagents to N-tert-butanesulfinyl imines proceeds readily at room temperature to afford the N-tert-butanesulfinyl-protected amine products in good yields and diastereomeric ratios. This method is functional group tolerant in both the imine substrate and benzyl zinc coupling partner. Moreover, benzyl zinc reagent addition to the N-tert-butanesulfinyl imine 3o prepared from isopropylidene-protected glyceraldehyde proceeds in high yield and with exceptional selectivity to provide rapid entry to hydroxyethylamine-based aspartyl protease inhibitors.(Figure Presented)
Intramolecular alkene carboamination reactions for the synthesis of enantiomerically enriched tropane derivatives
Schultz, Danielle M.,Wolfe, John P.
supporting information; experimental part, p. 2962 - 2965 (2011/07/07)
The synthesis of tropane derivatives via intramolecular Pd-catalyzed alkene difunctionalization reactions is described. Enantiopure N-aryl-γ- aminoalkenes bearing an aryl or alkenyl halide adjacent to the amino group were converted to benzo- or cycloalken
Highly diastereoselective reactions of 2-lithiated indoles with chiral N-tert-butanesulfinyl aldimines for the synthesis of chiral (2-indolyl) methanamine derivatives
Cheng, Liang,Liu, Li,Sui, Yong,Wang, Dong,Chen, Yong-Jun
, p. 1833 - 1843 (2008/02/12)
Nucleophilic addition reactions of 2-lithiated N-phenylsulfonylindoles with (R)-N-tert-butanesulfinyl aldimines provided chiral (2-indolyl) methanamine derivatives in moderate to good yields (up to 100%) with excellent diastereoselectivities (>99:1), in which no additional Lewis acids were required.
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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Page/Page column 53; 69, (2010/11/26)
The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.
