- BCL-2 INHIBITOR
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Disclosed herein is a compound of Formula (I) for inhibiting both Bcl-2 wild type and mutated Bcl-2, in particular, Bcl-2 G101V and D103Y, and a method of using the compound disclosed herein for treating dysregulated apoptotic diseases.
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Paragraph 0838-0842
(2021/10/22)
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- Group 4 dimethylsilylenebisamido complexes bearing the 6-[2-(diethylboryl) phenyl]pyrid-2-yl motif: Synthesis and use in tandem ring-opening metathesis/vinyl-insertion copolymerization of cyclic olefins with ethylene
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Two novel ZrIV- and HfIV-based bisamido complexes bearing the 6-[2-(diethylboryl)phenyl]pyrid-2-yl motif, that is, [ZrCl 2{Me2Si(DbppN)2}(thf)] (9) and [HfCl 2{Me2Si(DbppN)2
- Zou, Yuanlin,Wang, Dongren,Wurst, Klaus,Kuehnel, Christa,Reinhardt, Ingrid,Decker, Ulrich,Gurram, Venkatanavarana,Camadanli, Sebnem,Buchmeiser, Michael R.
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experimental part
p. 13832 - 13846
(2012/02/03)
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- 9,10-diarylanthracenes as molecular switches: Syntheses, properties, isomerisations and their reactions with singlet oxygen
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A series of 9,10-diarylanthracenes with various substituents at the ortho positions have been synthesised by palladium-catalysed cross-coupling reactions. Such compounds exhibit interesting physical properties and can be applied as molecular switches. Despite the high steric demand of the substituents, products were formed in moderate-to-good yields. In some cases, microwave conditions further improved yields. Bis-coupling afforded two isomers (syn and anti) that do not interconvert at room temperature. These products were easily separated and their relative stereochemistries were unequivocally assigned by NMR spectroscopy and X-ray analysis. The syn and anti isomers exhibit different physical properties (e.g., melting points and solubilities) and interconversion by rotation around the aryl-aryl axis commences at 300°C for alkyl- or alkoxy-substituted diarylanthracenes. The reactions with singlet oxygen were studied separately and revealed different reactivities and reaction pathways. The yields and reactivities depend on the size and electronic nature of the substituents. The anti isomers form the same 9,10-endoperoxides as the syn species, occasionally accompanied by unexpected 1,4-endoperoxides as byproducts. Thermolysis of the endoperoxides exclusively yielded the syn isomers. The interesting rotation around the aryl-aryl axis allows the application of 9,10-diarylanthracenes as molecular switches, which are triggered by light and air under mild conditions. Finally, the oxygenation and thermolysis sequence provides a simple, synthetic access to a single stereoisomer (syn) from an unselective coupling step.
- Zehm, Daniel,Fudickar, Werner,Hans, Melanie,Schilde, Uwe,Kelling, Alexandra,Linker, Torsten
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experimental part
p. 11429 - 11441
(2009/12/03)
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- Structure, conformation, and dynamic processes of the stereolabile atropisomers of hindered terphenyl hydrocarbons
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(Chemical Equation Presented) Ortho-substituted p-terphenyl hydrocarbons exist as trans and cis atropisomers that were identified by low-temperature NMR spectroscopy. The interconversion barriers increase with the dimensions of the ortho substituents, the experimental values being matched by ab initio calculations. X-ray diffraction shows that only the trans atropisomer is present in the solids. Spectra of a tert-butyl derivative in nonequilibrium conditions indicate that the cis is more populated than the trans atropisomer in solution, favored by attractive interactions.
- Lunazzi, Lodovico,Mazzanti, Andrea,Minzoni, Mirko,Edgar Anderson
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p. 1291 - 1294
(2007/10/03)
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- Substituted phenyl farnesyltransferase inhibitors
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Compounds of formula (I) or pharmaceutically acceptable salts thereof, inhibit farnesyltransferase. Methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
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- Efficient palladium-catalyzed N-arylation of indoles
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(Matrix presented) The N-arylation of indoles, including a variety of substituted ones, has been carried out using bulky, electron-rich phosphines as the supporting ligand in combination with Pd2(dba)3. Using this catalyst system, th
- Old, David W.,Harris, Michele C.,Buchwald, Stephen L.
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p. 1403 - 1406
(2007/10/03)
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- Highly active palladium catalysts for Suzuki coupling reactions
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Mixtures of palladium acetate and o-(di-tert-butylphosphino)biphenyl (4) catalyze the room-temperature Suzuki coupling of aryl bromides and aryl chlorides with 0.5-1.0 mol % Pd. Use of o-(dicyclohexylphosphino)biphenyl (2) allows Suzuki couplings to be carried out at low catalyst loadings (0.000001-0.02 mol % Pd). The process tolerates a broad range of functional groups and substrate combinations including the use of sterically hindered substrates. This is the most active catalyst system in terms of reaction temperature, turnover number, and steric tolerance which has been reported to date.
- Wolfe, John P.,Singer, Robert A.,Yang, Bryant H.,Buchwald, Stephen L.
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p. 9550 - 9561
(2007/10/03)
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