- Design and synthesis of potent N1-substituted indole melatonin receptor agonists.
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The design and expeditious synthesis of two new indole analogs with up to 5-fold potency of that of melatonin is described.
- Tsotinis, Andrew,Eleutheriades, Andreas,Hough, Katherine,Sugden, David
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- SUBSTITUTED BENZOAZEPINES AS TOLL-LIKE RECEPTOR MODULATORS
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Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.
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Page/Page column 61
(2012/07/28)
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- Convenient modification of the Leimgruber-Batcho indole synthesis: Reduction of 2-nitro-p-pyrrolidinostyrenes by the FeCl3-activated carbon-N2H4H2O system
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A new catalytic system containing ferric chloride, activated carbon, and hydrazine has been proposed for the reductive cyclization of β-dialkylamino-2-nitrostyrenes to give the corresponding indoles (Leimgruber-Batcho synthesis). Various substituted indoles may be obtained in high yield under these conditions.
- Taydakov,Dutova,Sidorenko,Krasnoselsky
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experimental part
p. 425 - 434
(2012/01/13)
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- Intermediates for indoles
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Ortho-nitrotoluenes are condensed with formamide acetals to yield the corresponding otho-nitro-β-aminestyrenes which undergo cyclization upon reduction to yield indoles.
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