- Silver-promoted regio- and stereoselective aminocyanation of alkynes for the synthesis of β-aminoacrylonitriles using N-isocyanoiminotriphenylphosphorane
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The silver-promoted intermolecular aminocyanation of alkynes for the synthesis of (Z)-β-aminoacrylonitriles is reported, using N-isocyanoiminotriphenylphosphorane (NIITP) as both the nitrile and amine source. The transformation proceeds in moderate to good yields, and in a regio- and stereoselective manner, using a wide range of acetylenes.
- Chen, Lingnan,Cao, Shanshan,Zhang, Jingping,Wang, Zikun
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supporting information
p. 1678 - 1681
(2019/05/29)
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- Blonanserin intermediate 4-fluorobenzoylacetonitrile synthesis method
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The invention provides a Blonanserin intermediate 4-fluorobenzoylacetonitrile synthesis method. The method comprises the following steps: (1) mixing acetonitrile, t-butanol, p-fluorobenzonitrile and organic solvent A into mixed solution; (2) adding potassium tert-butoxide and the organic solvent A to a reactor, then adding the mixed solution obtained in the step (1), and stirring for reaction to obtain 3-amino-3-p-fluorophenyl acrylonitrile; (3) hydrolyzing the 3-amino-3-p-fluorophenyl acrylonitrile with hydrochloric acid solution to obtain the 4-fluorobenzoylacetonitrile, wherein the organic solvent A is isopropyl ether and/or tetrahydrofuran. According to the method, the potassium tert-butoxide is used as a condensing agent, which greatly improves the safety of the process. The potassium t-butoxide is mild in nature, has hygroscopicity but is nonflammable, and can be used in wider temperature and humidity ranges, and is more conducive to industrial production. And meanwhile, the method is stable in yield and high in obtained product purity.
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Paragraph 0027; 0028; 0029; 0030; 0031; 0032; 0033-0065
(2017/09/02)
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- Rhodium-catalyzed asymmetric hydrogenation of β-acetylamino acrylonitriles
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The rhodium-catalyzed asymmetric hydrogenation of β-acetylamino acrylonitriles was investigated by using monophosphine and bisphosphine ligands. It was found that an Rh-QuinoxP complex exhibited high enantioselectivities for β-aryl substituted β-acetylamino acrylonitriles and the Rh-JosiPhos CyPF-t-Bu complex was proven to be effective for the hydrogenation of tetrasubstituted olefins from cyclic β-acetylamino acrylonitriles.
- Ma, Miaofeng,Hou, Guohua,Wang, Junru,Zhang, Xumu
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experimental part
p. 506 - 511
(2011/06/17)
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- FUROPYRIDINYL-SUBSTITUTED 1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF
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This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-l,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders
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Page/Page column 44
(2011/06/19)
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- Highly efficient RhI-catalyzed asymmetric hydrogenation of β-amino acrylonitriles
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(Figure Presented) It takes two to TangPhos: β-Amino acrylonitriles can be readily prepared from acetonitriles. Both of the E/Z isomers undergo hydrogenation with excellent enantioselectivity by using the Rh-TangPhos (TangPhos = l, 1'-ditert-butyl-(2, 2')-diphospholane) catalyst system. The products, chiral β-amino nitriles, are valuable chiral building blocks for many drugs.
- Ma, Miaofeng,Hou, Guohua,Sun, Tian,Zhang, Xiaowei,Li, Wei,Wang, Junru,Zhang, Xumu
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supporting information; experimental part
p. 5301 - 5304
(2010/09/08)
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- Modular routes towards new N,O-bidentate ligands containing an electronically delocalised β-enaminone chelating backbone
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Polyketones are synthesised by a transition-metal-catalysed copolymerisation of olefins and carbon monoxide. Nickel complexes with N,O-chelating ligands turned out to be promising catalysts in that field. In this work a series of new N,O ligands with an electronically delocalised β-enaminone backbone were synthesised and fully characterised. The ligand design was inspired by the ligand found in the most efficient nickel catalyst for polyketone synthesis and developed to a highly modular LEGO-like arsenal of reactions to versatile substituted β-enaminone ligands. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Beckmann, Udo,Eichberger, Eva,Lindner, Monika,Bongartz, Melanie,Kunz, Peter C.
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supporting information; experimental part
p. 4139 - 4147
(2009/04/11)
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- Heteroarylaminopyrazole derivatives useful for the treatment of diabetes
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The present invention relates to heteroarylaminopyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.
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Page/Page column 14
(2008/06/13)
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- A new expedient route to 2,6-diaryl-3-cyano-4- (trifluoromethyl)pyridines
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1-Aryl-4,4,4-trifluoro-1,3-butanediones 1 react with β-amino-β- arylacrylonitrile 2, readily available from acetonitrile with aryl nitriles in the presence of potassium t-butoxide, to afford the corresponding 2,6- diaryl-3-cyano-4-(trifluoromethyl)pyridin
- Yamaguchi,Katsuyama,Funabiki,Matsui,Shibata
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p. 805 - 810
(2007/10/03)
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- Potential antiarthritic agents. II. Benzoylacetonitriles and β-aminocinnamonitriles
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Benzoylacetonitrile and β-aminocinnamonitrile are shown to possess potent intiinflammatory activity in the rat adjuvant arthritis model. In a series of phenyl-substituted analogues, only o-, m-, and p-fluorobenzoylacetonitrile and m- and p-fluoro-β-aminocinnamonitrile retained activity. Additionally, β-amino-2- and β-amino-3-thiopheneacrylonitrile and β-oxo-2- and β-oxo-3-thiophenepropionitrile exhibited similar activity. These agents are not believed to be acting via prostaglandin synthetase inhibition. The metabolic profile of benzoylacetonitrile is also described.
- Ridge,Hanifin,Harten,Johnson,Menschik,Nicolau,Sloboda,Watts
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p. 1385 - 1389
(2007/10/09)
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- β Aminocinnamonitriles as potential antiinflammatory agents
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A number of β aminocinnamonitriles have been prepared by the reaction of salts of acetonitrile and proprionitrile with benzonitrile. These materials were evaluated in the carrageenan antiinflammatory screen in Royal Hart, Wistar strain rats. Despite food weight gains with the parent molecule, β aminocinnamonitrile, only marginal activity was found in related compounds and some possible 'metabolites'.
- Lang Jr.,Cohen
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p. 441 - 443
(2007/10/08)
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