CAS: 14150-95-9; 2-Aminopyridine 1-Oxide

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专利信息

专利号:US-8076479-B2
优先权日:2006-08-28
标题 :Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates
发明人：CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI
权利人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI; SCHERING CORP
摘要:Disclosed is a process for the synthesis of compounds of Formula I n nby sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,n n nwherein R 1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R 2a —OH), R 2a is a linear, branched or cyclic alkyl group, R 2 is a linear, branched or cyclic alkyl group, and R 3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1,n n nwith a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.

专利号:US-3886180-A
优先权日:1973-03-15
标 题:Process for the synthesis of N-hydroxypyrroles
发明人：ABRAMOVITCH RUDOLPH ABRAHAM; CUE JR BERKELEY WENDELL
权利人:ABRAMOVITCH RUDOLPH ABRAHAM; CUE JR BERKELEY WENDELL
摘要:A process is described for the preparation of N-hydroxypyrrole2-carbonitriles, N-hydroxyimidazole-2-carbonitriles, pyrrole-2carbonitriles, and 3-substituted-2, 3-dihydro-2-pyrrolones by thermally decomposing 2-azidoheteroaromatic N-oxides. In the process a 2-azidoheteroaromatic N-oxide is heated in a suitable solvent for a period of time sufficient to bring the reaction to completion. Removal of the solvent by conventional methods gives the desired product. Which product is obtained is determined by the choice of solvents. In non-polar aprotic solvents, Nhydroxypyrrole-2-carbonitriles or N-hydroxyimidazole-2carbonitriles are obtained. In nucleophilic solvents capable of undergoing Michael-type additions pyrrole-2-carbonitriles, imidazole-2-carbonitriles, and 3-substituted-2,3-dihydro-2pyrrolone derivatives are obtained where a solvent molecule comprises the 3-substituent. These compounds are useful as antibaterials, e.g., against E. Coli.

专利号:US-4006160-A
优先权日:1973-03-15
标题:Process for the synthesis of N-hydroxypyrroles, N-hydroxyimidazoles, and derivatives thereof
发明人：ABRAMOVITCH RUDOLPH ABRAHAM; CUE JR BERKELEY WENDELL
权利人:UNIV ALABAMA
摘要:A process is described for the preparation of N-hydroxypyrrole-2-carbonitriles, N-hydroxyimidazole-2-carbonitriles, pyrrole-2-carbonitriles, and 3-substituted-2, 3-dihydro-2-pyrrolones by thermally decomposing 2-azidoheteroaromatic N-oxides. In the process a 2-azidoheteroaromatic N-oxide is heated in a suitable solvent for a period of time sufficient to bring the reaction to completion. Removal of the solvent by conventional methods gives the desired product. Which product is obtained is determined by the choice of solvents. In non-polar aprotic solvents, N-hydroxypyrrole-2-carbonitriles or N-hydroxyimidazole-2-carbonitriles are obtained. In nucleophilic solvents capable of undergoing Michael-type additions pyrrole-2-carbonitriles, imidazole-2-carbonitriles, and 3-substituted-2,3-dihydro-2-pyrrolone derivatives are obtained where a solvent molecule comprises the 3-substituent. These compounds are useful as anti-bacterials, e.g., against E. Coli.

专利号:US-7022846-B2
优先权日:2002-06-10
标 题 :Metabolites of prinomastat and their synthesis
发明人：OUELLETTE MICHAEL A; POTTS BARBARA C M; SRIRANGAM JAYARAM K; TIBBETTS ANTHONY R; ZHANG KANYIN E
权利人:AGOURON PHARMA
摘要:Metabolites of a matrix metalloproteinase inhibitor prinomastat and their synthesis. These metabolites are: (3S)-N-hydroxy-4-(4-((1-oxy-pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl-tetrahydro-2H-1,4-thiazine-3-carboxamide (M6); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(1-oxy-pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M7); (3S)-2,2-dimethyl-4-[4-(1-oxypyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M8); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M2); and (3S)-2,2-dimethyl-4-[4-(pyridin-4yloxy)-benzenesulfonyl)-thiomorphpline-3-carboxylic acid amide (M3).

专利号:US-4118384-A
优先权日:1976-02-21
标题 :Process for preparation of azo dyestuffs by coupling in presence of aromatic sulphonic acid-formaldehyde reaction product
发明人：MOLLS HANS-HEINZ; SCHIWY WILLY; HORNLE REINHOLD; NEBELING REINHARD
权利人:BAYER AG
摘要:Dyestuff dispersions and dyestuff solutions free from salt or at least having a low salt content are obtained in that the diazotization is carried out with addition of free dispersing agent acid to which, after the synthesis, either no basic agents are added or basic agents are added only up to a pH value of 3. The disclosed process gives dyestuff compositions of low salt content and results in readily dispersible dyestuffs when water insoluble dyestuffs are prepared and stable solutions when water soluble dyestuffs are prepared. The process is widely applicable and chemical constitution of the dyestuffs is conventional.

专利号:US-2008058518-A1
优先权日:2006-08-28
标 题 :Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates