- Facile synthesis of 3-trimethylsilylindazoles by [3+2]cycloaddition reaction of lithium trimethylsilyldiazomethane with benzynes
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[3+2]Cycloaddition reaction of lithium trimethylsilyldiazomethane with benzynes, generated from halobenzenes, gave the corresponding 3-trimethylsilylindazoles in good to moderate yields.
- Shoji, Yoshimichi,Hari, Yoshiyuki,Aoyama, Toyohiko
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Read Online
- An Effective Method for the Synthesis of 1,3-Dihydro-2H-indazoles via N-N Bond Formation
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The [4+1] cycloaddition reaction of bifunctional amino reagents has been achieved with in situ formed aza-ortho-quinone methides. Specifically, N-(tosyloxy)carbamates were used as an N1 synthon and bifunctional amino reagents for this transformation, which provides a metal-free, catalyst-free, and oxidant-free strategy to form nitrogen-nitrogen bonds. (Figure presented.).
- Zhang, Xiaoke,Pan, Yang,Liang, Peng,Ma, Xiaofeng,Jiao, Wei,Shao, Huawu
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p. 5552 - 5557
(2019/11/22)
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- NOVEL CATALYSTS
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The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.
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Page/Page column 60
(2012/06/01)
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- Palladium-catalyzed cross-coupling of aryl chlorides and tosylates with hydrazine
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Hydrazine is not a problem anymore: The title transformation is the first reaction to yield aryl hydrazines through the cross-coupling of aryl chlorides and tosylates with hydrazine. An appropriately designed palladium catalyst allows this reaction to proceed rapidly under mild conditions, and with excellent chemoselectivity (see scheme; Ad=adamantyl, Ts=4-toluenesulfonyl).
- Lundgren, Rylan J.,Stradiotto, Mark
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supporting information; experimental part
p. 8686 - 8690
(2011/01/08)
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- Toward biophysical probes for the 5-HT3 receptor: Structure-activity relationship study of granisetron derivatives
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This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT3A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identification of positions on the granisetron core that might be used as attachment points for biophysical tags. A BODIPY fluorophore was appended to one such position and specifically bound to 5-HT3A receptors in mammalian cells.
- Vernekar, Sanjeev Kumar V.,Hallaq, Hasan Y.,Clarkson, Guy,Thompson, Andrew J.,Silvestr, Linda,Lummis, Sarah C. R.,Lochner, Martin
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supporting information; experimental part
p. 2324 - 2328
(2010/07/17)
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- INDOLE, INDAZOLE, AND BENZAZOLE DERIVATIVE
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The compound of the formula (I): wherein W is a group of the following formula (VIII) binding to any possible position on the Q: Q is, together with W, a group of the formula: -C(M=C(R3A)-N(R3)-, etc.; R3A is H or optionally substituted lower alkyl; R4, R5, R6, and R7 are independently H or optionally substituted lower alkyl; R1 is optionally substituted lower alkyl, etc.; R2 is H, etc.; R3 is H, etc.; Ar is phenyl, etc., or a pharmaceutically acceptable salt thereof, where these compounds exhibiting β3-adrenoceptor-stimulating activity and being useful as a medicament for treatment of obesity, etc.
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Page/Page column 83
(2010/02/11)
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- Inhibition of neuronal nitric oxide synthase by 7-methoxyindazole and related substituted indazoles
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The synthesis and pharmacological evaluation of methoxyindazoles as new inhibitors of neuronal nitric oxide synthase are presented. The 7-methoxyindazole, although less potent than 7-NI, is the most active compound of the series in an in vitro enzymatic assay of neuronal nitric oxide synthase activity. This result shows that the nitro-substitution is not indispensable to the biological activity of the indazole ring. 7-Methoxyindazole possesses in vivo NOS inhibitory as well and related antinociceptive properties.
- Schumann, Pascale,Collot, Valerie,Hommet, Yannick,Gsell, Willy,Dauphin, Francois,Sopkova, Jana,MacKenzie, Eric T.,Duval, Dominique,Boulouard, Michel,Rault, Sylvain
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p. 1153 - 1156
(2007/10/03)
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