- Rapid and Simple Access to α-(Hetero)arylacetonitriles from Gem-Difluoroalkenes
-
A scalable cyanation of gem-difluoroalkenes to (hetero)arylacetonitrile derivatives was developed. This strategy features mild reaction conditions, excellent yields, wide substrate scope, and broad functional group tolerance. Significantly, in this reacti
- Hu, Dandan,Liu, Jiayue,Ren, Hongjun,Song, Jinyu,Zhang, Jun-Qi,Zhu, Guorong
-
supporting information
p. 786 - 790
(2022/01/28)
-
- Copper-Catalyzed Cyanation of N-Tosylhydrazones with Thiocyanate Salt as the "cN" Source
-
A novel protocol for the synthesis of α-aryl nitriles has been successfully achieved via a copper-catalyzed cyanation of N-tosylhydrazones employing thiocyanate as the source of cyanide. The features of this method include a convenient operation, readily available substrates, low-toxicity thiocyanate salts, and a broad substrate scope.
- Huang, Yubing,Yu, Yue,Zhu, Zhongzhi,Zhu, Chuanle,Cen, Jinghe,Li, Xianwei,Wu, Wanqing,Jiang, Huanfeng
-
p. 7621 - 7627
(2017/07/26)
-
- PRODUCTION OF INDUCED PLURIPOTENT STEM CELLS
-
The present disclosure relates to methods and compositions that improve the in vitro production of induced pluripotent stem cells through the use of compounds that promote degradation of p53. The disclosure also relates to compositions and methods for the treatment of cancer, pancreatitis and intracellular pathogens.
- -
-
Page/Page column 63
(2012/06/30)
-
- POTENT SMALL MOLECULE INHIBITORS OF AUTOPHAGY, AND METHODS OF USE THEREOF
-
Certain aspects of the invention relates to small molecule autophagy inhibitors, and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity.
- -
-
Page/Page column 57
(2011/02/24)
-
- SUBSTITUTED AROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
-
The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions (formula (I)).
- -
-
Page/Page column 131; 132
(2010/11/18)
-
- 3-benzyl-1,2,4-triazolo[4,3-α] pyrazines
-
3-benzyl-1,2,4-triazolo [4,3-α] pyrazines are prepared. They are useful as anticonvulsants.
- -
-
-
- ELECTRFLUORATION EN POSITION BENZYLIQUE DANS LE SULFOLANE
-
The use of sulfolane as a solvent instead of acetonitrile in the electrofluorination of benzylic derivatives 1, (R=H, Cl) gives greater yields of benzylic fluorides 2, since the formation of acetamide byproducts 4 is prevented.However, the parallel fluorination of the aromatic nucleus is not avoided under these conditions.
- Laurent, Eliane,Marquet, Bernard,Tardivel, Robert
-
p. 115 - 126
(2007/10/02)
-
- Photochemical Aromatic Cyanomethylation: Aromatic Substitution by Way of Radical Cations
-
Photolysis at 254 nm of chloroacetonitrile in the presence of aromatic hydrocarbons led to ring cyanomethylation.In addition radical coupling products were found, especially with toluene where 3-phenylpropionitrile, succinonitrile, and bibenzyl accompanied the tolylacetonitriles.These same byproducts were obtained from toluene and chloroacetonitrile upon thermolysis with peroxide initiators, but no nuclear cyanomethylation was observed.The mechanism for aromatic cyanomethylation involves initial excitation of the aromatic hydrocarbons, followed by an electron transfer (probably by way of an exiplex) to chloroacetonitrile, which was found to quench aromatic fluorescence at high rates.Direct spectral evidence for the resulting radical cation with p-dimethoxybenzen was obtained by using flash laser spectroscopy.Loss of a chloride ion from the resulting radical anion produces a cyanomethyl radical in close proximity to an aromatic radical cation.Coupling leads to the aromatic substitution products whereas radicals escaping from the cage account for the observed byproducts.
- Kurz, M. E.,Lapin, S. C.,Miriam, K.,Hagen, T. J.,Qian, X. Q.
-
p. 2728 - 2733
(2007/10/02)
-
- Photochemical Aromatic Cyanomethylation
-
Cyanomethylation is accomplished by the photolysis of chloroacetonitrile in the presence of aromatics by way of electron transfer followed by radical coupling.
- Lapin, Stephen,Kurz, Michael E.
-
p. 817 - 818
(2007/10/02)
-
