- Method for synthesizing netarsudil intermediate
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The invention relates to a method for synthesizing a netarsudil intermediate that is 6-aminoisoquinoline. The method includes (1) dissolving 2-bromo-2-methylpropionic acid; (2) adding oxalyl chloride,and then reacting the mixture; (3) after the reaction is completed, pouring the reaction solution into aqueous ammonia, stirring the mixture, performing filtration and drying a product. The method utilizes conventional and easily available chemical materials, and has characteristics of mild reactions, a short route and a high yield.
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Paragraph 0067; 0083-0087; 0088; 0104-0108; 0109; 0126-0130
(2019/11/20)
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- Methods for the preparation of 6-aminoisoquinoline
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Described are methods for the preparation of 6-aminoisoquinoline, a useful intermediate compound in the synthesis of kinase inhibitors.
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Page/Page column 21; 22
(2018/01/21)
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- Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents
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The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
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Page/Page column 307
(2015/11/16)
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- Solid supported rhodium(0) nanoparticles: An efficient catalyst for chemo- and regio-selective transfer hydrogenation of nitroarenes to anilines under microwave irradiation
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A Solid-supported rhodium(0) (SS-Rh) catalyst has been developed and applied for the chemo- and regio-selective reduction of nitroarenes functionalized with CC multiple bonds and dinitroarenes to their corresponding amines respectively using hydrazine hydrate (N2H4· H2O) as a reducing source under mild microwave irradiation (MWI) conditions. The present methodology also shows excellent compatibility with a broad range of structurally diverse reducible functional groups. The catalyst can be recovered by simple filtration and reused for 13 cycles with consistent activity hence reduces the cost of the catalyst assertively.
- Guha, Nitul Ranjan,Bhattacherjee, Dhananjay,Das, Pralay
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supporting information
p. 2912 - 2916
(2014/05/06)
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- NOVEL SELECTIVE ANDROGEN RECEPTOR MODULATORS
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The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl,etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; Q is —CO—, —(CH2)q—, —(CHRs)q—, or (CRsRt)q—, where Rs and Rt are independently C1-C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.
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Page/Page column
(2014/06/23)
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- SUBSTITUTED ISOQUINOLINE DERIVATIVE
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The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the
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Page/Page column 8
(2012/02/15)
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- Phosphane-free green protocol for selective nitro reduction with an iron-based catalyst
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Iron phthalocyanine with iron sulfate has been successfully applied for high chemo- and regioselective reduction of aromatic nitro compounds to give the corresponding amines in a green solvent system without using any toxic ligand. The catalytic systems were also compatible with a large range of other reducible functional groups, such as keto, acid, amide, ester, halogen, lactone, nitrile, N-benzyl, O-benzyl, hydroxy, and heterocycles. In the present study, dinitro compounds have been regioselectively reduced to the corresponding amines with high yield. In most of the cases the conversion and selectivity was greater than 99% as determined by GC-MS analysis. Copyright
- Sharma, Upendra,Verma, Praveen Kumar,Kumar, Neeraj,Kumar, Vishal,Bala, Manju,Singh, Bikram
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experimental part
p. 5903 - 5907
(2011/06/20)
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- Highly chemo- and regioselective reduction of aromatic nitro compounds catalyzed by recyclable copper(II) as well as cobalt(II) phthalocyanines
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Copper/cobalt phthalocyanines were established for the first time as catalysts for the very efficient chemo- and regioselective reduction of aromatic nitro compounds to generate the corresponding amines. The selective reduction of nitro compounds was observed in the presence of a large range of functional groups such as aldehyde, keto, acid, amide, ester, halogen, lactone, nitrile and heterocyclic functional groups. Furthermore, the present method was found to be highly regioselective towards the reduction of aromatic dinitro compounds in a short time with high yields. In most of the cases the conversion and selectivity were >99% as monitored by GC-MS. The reduction mechanism was elucidated by UV-vis and electrospray ionization quadrupole time-of-flight tandem mass spectrometry.
- Sharma, Upendra,Kumar, Praveen,Kumar, Neeraj,Kumar, Vishal,Singh, Bikram
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experimental part
p. 1834 - 1840
(2010/10/21)
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- Ultrasound-promoted highly efficient reduction of aromatic nitro compounds to the aromatic amines by samarium/ammonium chloride
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Ultrasound-promoted, highly efficient reduction of several aromatic nitro compounds to the aromatic amines was achieved by samarium/ammonium chloride mediated reaction. (C) 2000 Elsevier Science Ltd.
- Basu, Manas K.,Becker, Frederick F.,Banik, Bimal K.
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p. 5603 - 5606
(2007/10/03)
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- Pharmaceutically active compounds
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The invention relates to a class of tetrahydroisoquinolinylalkanoic acids containing an aryl sulphonamide group which have activity as thromboxane A2 antagonists.
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