- Compound and application thereof
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The invention provides a novel compound. The novel compound has certain inhibitory activity for indoleamine 2,3-dioxygenase (IDO) which is oxido-reductase, and accordingly the novel compound can be used for treating diseases related to the indoleamine 2,3-dioxygenase and can be applied to cancer and immunity related diseases.
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- Efficient copper-catalyzed N-arylations of nitrogen-containing heterocycles and aliphatic amines in water
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A simple and efficient copper-catalyzed method has been developed for N-arylations of nitrogen-containing heterocycles and aliphatic amines in water. The protocol uses (1E,2E)-oxalaldehyde dioxime (OADO) as the ligand, and water as the solvent, and shows good tolerance towards various functional groups.
- Li, Xufeng,Yang, Daoshan,Jiang, Yuyang,Fu, Hua
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experimental part
p. 1097 - 1105
(2010/08/06)
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- A mild and efficient method for copper-catalyzed Ullmann-type N-arylation of aliphatic amines and amino acids
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An efficient and general protocol for copper-catalyzed N-arylation of aliphatic amines and amino acids has been developed using aryl iodides under mild conditions (coupling temperature at 25-35°C). For the N-(o-nitrophenyl) amino acid derivatives, subsequent reduction of the nitro group in the presence of tin(II) chloride resulted in 3,4-dihydroquinoxalin-2(1H)-one derivatives in good yields. Georg Thieme Verlag Stuttgart New York.
- Jiang, Qun,Jiang, Deshou,Jiang, Yuyang,Fu, Hua,Zhao, Yufen
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p. 1836 - 1842
(2008/02/10)
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- Kinetics and mechanism of thermal gas-phase elimination of α- and β- (N-arylamino)propanoic acid: Experimental and theoretical analysis
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2-(N-Phenylamino)propanoic acid 1a and 3-(N-phenylamino)-propanoic acid 2a together with four of their aryl analogues were pyrolysed in the gas-phase. The reactions were homogeneous and free from catalytic and radical pathways. Analysis of the pyrolysate of 1 showed the elimination products to be carbon monoxide, acetaldehyde and aniline, while the pyrolysate of 2 reveals the formation of acrylic acid in addition to aniline. Theoretical study of the pyrolysis of 2 using an ab initio SCF method lend support to a reaction pathway involving a 4-membered cyclic transition state.
- Al-Awadi, Sundus A.,Abdallah, Mariam R.,Hasan, Mohamad A.,Al-Awadi, Nouria A.
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p. 3045 - 3049
(2007/10/03)
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- Isosteres of chiral clofibric acid analogs: Synthesis, resolution, absolute configuration and HPLC detection of the optical purity
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Both racemic and enantiomeric forms of some isosteres of chiral clofibric acid analogs have been synthesized. Also, the absolute configuration has been established by chemical correlation and the optical purity determined by a simple HPLC procedure. Moreover, these studies show that the isosteric substitution of the ether oxygen atom of α-aryloxy- alkanoic acids with sulfur, amino and methylene groups lead to compounds in which both biological activity and stereoselectivity regarding chloride channel are highly reduced.
- Ferorelli,Loiodice,Tortorella,Amoroso,Bettoni,Conte- Camerino,De Luca
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p. 367 - 374
(2007/10/03)
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- IMINE CHEMISTRY-II.A NEW ROUTE TO CYCLIC ENAMINONES FROM IMINES AND β-PROPIOLACTONE OR α,β-UNSATURATED ACIDS. THE PREPARATION OF ENAMINO-THIONES
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Imines, formed from cyclohexanone and primary aromatic and aliphatic amines, were reacted with β-propiolactone, acrylic, crotonic, and methacrylic acids to give as main products bicyclic lactams, 3,4,5,6,7,8-hexahydro-2-quinolinone, 2, and enaminones, 2,3,5,6,7,8-hexahydro-4-quinolinone, 3.The enaminones 3 and a series of noncyclic enaminones 11 were reacted with 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane-2,4-disulfide, 9, a new thiation reagent, giving the corresponding enamino-thiones 10 and 12, respectively.Compound 2a was also reacted with 9 giving N-phenyl- 3,4,5,6,7,8-hexahydro-2-quinolinthione, 13a. 360 MHz (1)H NMR and 90.25 MHz (13)C NMR data are reported for the compounds 2a, 3a and 10a.
- Shabana, R.,Rasmussen, J. B.,Olesen, S. O.,Lawesson, S.-O.
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p. 3047 - 3051
(2007/10/02)
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