- SYNTHESIS OF 20-NOR-SALVINORIN A
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The invention provides 20-nor-salvinorin A, an analog of the kappa-opioid agonist salvinorin A. The 20-nor-salvinorin A is an active kappa-opioid modulator and can be used for treatment of medical conditions wherein modulation of the kappa-opioid receptor
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Page/Page column 19; 21
(2019/01/07)
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- A highly efficient metal-free approach to: Meta - And multiple-substituted phenols via a simple oxidation of cyclohexenones
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A novel and efficient metal-free approach to substituted phenols has been disclosed from simple and readily available cyclohexenones and cyclohexenone equivalents. Dimethyl sulfoxide (DMSO), a simple and common organic reagent, was employed as a mild oxidant in this I2-catalysis, which significantly tolerates various substituents including some easily oxidizable or reducible functionalities. The challenging meta- and multiple-substituted phenols could be well prepared by this method. The metal-free and mild oxidation make this protocol very simple, practical, and easy to handle.
- Liang, Yu-Feng,Song, Song,Ai, Lingsheng,Li, Xinwei,Jiao, Ning
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supporting information
p. 6462 - 6467
(2018/06/08)
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- THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
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The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
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- THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
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The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r are as defi
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- THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
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The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, and t are as
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- TRIAZOLYL DERIVATIVES AS SYK INHIBITORS
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Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
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- THIAZOLE-SUBSTITUTED AMINOPYRIMIDINES AS SPLEEN TYROSINE KINASE INHIBITORS
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The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provid
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- THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
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The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
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- BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS
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The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
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- Diaxial diureido decalins as compact, efficient, and tunable anion transporters
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Decalins bearing two axial -NHCONHAr substituents and an ester-linked alkyl side chain have been synthesized and studied as anion receptors and transporters. The design relates to steroid-based cholapods but is more compact and less intrinsically lipophil
- Hussain, Sabir,Brotherhood, Peter R.,Judd, Luke W.,Davis, Anthony P.
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supporting information; experimental part
p. 1614 - 1617
(2011/04/17)
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- High-yielding synthesis of Nefopam analogues (functionalized benzoxazocines) by sequential one-pot cascade operations
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An efficient amine-/ruthenium-catalyzed three-step process for the synthesis of Nefopam analogues was achieved through combinations of cascade enamine amination/iso-aromatization/allylation and diene or enyne metathesis as key steps starting from functionalized Hagemann's esters. In this communication, we discovered the application of ruthenium-catalysis on olefins containing free amines without in situ formation of salts.
- Ramachary, Dhevalapally B.,Narayana, Vidadala V.,Prasad, M. Shiva,Ramakumar, Kinthada
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body text
p. 3372 - 3378
(2010/01/06)
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- Organocatalytic cascade reactions based on push-pull dienamine platform: Synthesis of highly substituted anilines
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(Chemical Equation Presented) A practical and novel one-pot organocatalytic selective process for the cascade synthesis of highly substituted o-hydroxydiary lamines and o-pyrrolidin-1-yldiarylamines is reported. Direct combination of amine-catalyzed cascade Knoevenagel/Michael/aldol condensation/decarboxylation and cascade enamine amination/isoaromatization of alkyl acetoacetates, aldehydes, and nitrosoarenes furnished the highly functionalized anilines with high yields.
- Ramachary, Dhevalapally B.,Ramakumar, Kinthada,Narayana, Vidadala V.
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p. 1458 - 1463
(2007/10/03)
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- Solvent-free robinson annelation reaction
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Solvent-free Robinson annelation reaction proceeded at room temperature to give corresponding cyclohexenones.
- Miyamoto, Hisakazu,Kanetaka, Shotaro,Tanaka, Koichi,Yoshizawa, Kazuhiro,Toyota, Shinji,Toda, Fumio
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p. 888 - 889
(2007/10/03)
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- Stereospecific total synthesis of amberketal and a homologue
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Amberketal (1a) and acetal homologue (2a) have been synthesised from a commercially available methyl acetoacetate involving palladium catalysed cyclisation as a key step.
- Kongkathip, Boonsong,Kongkathip, Ngampong,Janthorn, Sirinan,Virarangsiyakorn, Duangmanee
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- A New Annulation Reagent, 2-Oxo-3-alkenylphosphonates. Reactions with Carbonyl-Stabilized Carboanions or Silyl Enol Ethers Leading to Cyclohexanones
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The reactions of 2-oxo-3-alkenylphosphonates with carbonyl-stabilized carbanions directly lead to 2-cyclohexen-1-ones through a sequence of Michael reaction and intramolecular Horner-Emmons olefination.On the other hand, the Lewis acid-mediated reactions with silyl enol ethers produce 1,5-diketones as Michael adducts, which then undergo cyclization on treatment with sodium hydride or triethylamine/zinc (II) bromide to afford 2-cyclohexen-1-ones or 2-phosphinyl-2-cyclohexen-1-ones, respectively.
- Wada, Eiji,Funakoshi, Junji,Kanemasa, Shuji
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p. 2456 - 2464
(2007/10/02)
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