- A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus–Silane System
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A simple and direct approach for the regioselective construction of the privileged 2H-indazole scaffold is described. The developed one-pot strategy involves phospholene-mediated N?N bond formation to access 2H-indazoles. The amount of organophosphorus reagent was minimized by recycling the phospholene oxide with organosilane reductants. Starting from functionalized 2-nitrobenzaldehydes and primary amines, a mild reductive cyclization, involving the use of commercially available phospholene oxide and silanes, delivered a wide variety of substituted 2H-indazoles in good to excellent yields.
- Schoene, Jens,Bel Abed, Hassen,Schmieder, Peter,Christmann, Mathias,Nazaré, Marc
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supporting information
p. 9090 - 9100
(2018/06/29)
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- GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS
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The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
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Paragraph 00276
(2016/07/05)
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- COVALENT INHIBITORS OF KRAS G12C
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Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
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- Synthesis of calothrixins and its analogs using FeCl3-mediated domino reaction protocol
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A novel one pot synthesis of calothrixin B and its analogs is achieved involving an FeCl3-mediated domino reaction of enamines in dry DMF at reflux. Alternatively, the enamines upon interaction with CuBr2 in DMF at reflux led to the
- Ramalingam, Bose Muthu,Saravanan, Velu,Mohanakrishnan, Arasambattu K.
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supporting information
p. 3726 - 3729
(2013/08/23)
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- Synthesis and biological evaluation of 4,5-dihydro-1H-pyrazole derivatives as potential nNOS/iNOS selective inhibitors. Part 2: Influence of diverse substituents in both the phenyl moiety and the acyl group
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In a preliminary article, we reported a series of 4,5-dihydro-1H-pyrazole derivatives as neuronal nitric oxide synthase (nNOS) inhibitors. Here we present the data about the inhibition of inducible nitric oxide synthase (iNOS) of these compounds. In gener
- Carrión, M. Dora,Chayah, Mariem,Entrena, Antonio,López, Ana,Gallo, Miguel A.,Acu?a-Castroviejo, Darío,Camacho, M. Encarnación
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p. 4132 - 4142
(2013/07/25)
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- Novel benzofurans and indols
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Compounds of formula (I) wherein X is a fluorine or a chlorine atom; the methyl groups located at the 2- and 5-position of the piperazine ring are in trans-configuration to each other; Y is NH or O; R1 is selected front hydrogen, chloro, bromo,
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Page/Page column 6
(2008/06/13)
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- Synthesis and regioselective ribosylation of 6,7-dichloroimidazo[4,5- b]quinolin-2-one
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The polyhalogenated benzimidazole nucleosides 2,5,6-trichloro-1-(β-D- ribofuranosyl)benzimidazole (TCRB) and the 2-bromo analogue (BDCRB) were synthesized in our laboratory and established as potent and selective antiviral agents against human cytomegalovirus (HCMV) with a novel mode of action. In an effort to study the behavior of the key substructure of these analogues in a dimensionally stretched-out manner and probe the spatial limitation of the target enzyme(s), a series of N1- and N3-ribonucleosides of imidazo[4,5-b]quinolines were designed as linear dimensional analogues. The nucleosides 6,7-dichloro-1-(β-D-ribofuranosyl)imidazo[4,5-b]quinolin-2-one and 6,7-dichloro-3-(β-D-ribofuranosyl)imidazo[4,5-b]quinolin-2-one were selected and prepared as the key intermediates in this study. During this study, a novel photoassisted annulation was developed for the synthesis of 6,7-dichloroimidazo[4,5-b]quinolin-2-one, which overcame several problems that were encountered with the literature annulation method. Regioselective ribosylations of this heterocycle were developed and gave both the N1 and the N3 isomers in high yield.
- Zhu, Zhijian,Lippa, Blaise,Townsend, Leroy B.
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p. 4159 - 4168
(2007/10/03)
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