- Intramolecular Pd-catalyzed reductive amination of enolizable sp3-C-H bonds
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A palladium-catalyzed reductive cyclization of nitroarenes has been designed to construct sp3-C-NHAr bonds from sp3-C-H bonds by using an enolizable nucleophile to intercept a nitrosoarene intermediate. Exposure of ortho-substituted nitroarenes to 5 mol ?% of Pd(OAc)2 and 10 mol ?% of phenanthroline under 2 atm of CO constructs partially saturated 5-, 6-, or 7-membered N-heterocycles using α-pyridyl carboxylates, malonates, 1,3-dimethylbarbituric acid, 1,3-diones, or difurans as the nucleophile.
- Ford, Russell L.,Alt, Isabel,Jana, Navendu,Driver, Tom G.
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p. 8827 - 8831
(2019/10/28)
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- HETEROCYCLIC SULFONAMIDES AS INHIBITORS OF TRANSFER RNA SYNTHETASE FOR USE AS ANTIBACTERIAL AGENTS
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The present invention provides aromatic sulphonamides as tRNA synthetase inhibitors and process for their synthesis, pharmaceutical composition and method for treatment. Compounds disclosed can be used as antibacterial agents for the treatment or prevention of conditions caused by or contributed by aerobic and anaerobic Gram-positive pathogens, more particularly against bacterium, for example Staphylococcus, Enterococci and Streptococci. Compounds disclosed are used in particular for the treatment of skin and soft tissue infection, Formula (I)
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Page/Page column 13-14
(2012/02/13)
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- Synthetic studies on indolocarbazoles: Total synthesis of staurosporine aglycon
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A synthesis of staurosporine aglycon and its analogs was achieved in a 28-36% overall yield starting from 2-methylindole. The prominent key steps for the synthesis of the indolocarbazole alkaloids involved electrocyclization and nitrene insertion reactions.
- Rajeshwaran, Ganesan Gobi,Mohanakrishnan, Arasambattu K
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supporting information; experimental part
p. 1418 - 1421
(2011/05/04)
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- Bicyclic And Tricyclic Compounds As KAT II Inhibitors
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Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
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Page/Page column 26-27
(2010/12/31)
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- SUBSTITUTED 7-SULFANYLMETHYL-, 7-SULFINYLMETHYL- AND 7-SULFONYLMETHYLINDOLES AND THE USE THEREOF
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The present application relates to novel 7-sulfanylmethyl-, 7-sulfinylmethyl- and 7-sulfonylmethylindole derivatives, processes for the preparation thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases, and the use thereof for the manufacture of medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
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Page/Page column 30
(2010/05/13)
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- Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors
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Cyclin-dependent kinase 5 (CDK5) is a serine/threonine kinase that plays a critical role in the early development of the nervous system. Deregulation of CDK5 is believed to contribute to the abnormal phosphorylation of various cellular substrates associated with neurodegenerative disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. Acyclic urea 3 was identified as a potent CDK5 inhibitor and co-crystallographic data of urea 3/CDK2 enzyme were used to design a novel series of 3,4-dihydroquinazolin-2(1H)-ones as CDK5 inhibitors. In this investigation we present our synthetic studies toward this series of compounds and discuss their biological relevance as CDK5 inhibitors.
- Rzasa, Robert M.,Kaller, Matthew R.,Liu, Gang,Magal, Ella,Nguyen, Thomas T.,Osslund, Timothy D.,Powers, David,Santora, Vincent J.,Viswanadhan, Vellarkad N.,Wang, Hui-Ling,Xiong, Xiaoling,Zhong, Wenge,Norman, Mark H.
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p. 6574 - 6595
(2008/03/27)
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- 2, 3, 4, 5-TETRAHYDRO-1H-[1, 4] BENZODIAZEPINE-3-HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE INHIBITORS
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Compounds having formula (1) are useful in treating disease conditions mediated by matrix metalloproteinases and TACE, such as tumor growth, osteoarthritis, rheumatoid arthritis and degenerative cartilage loss.
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- 2,3,4,5-tetrahydro-1H-(1,4)benzodiazepine-3-hydroxamic acids
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Compounds having the following formula: ? are useful in treating disease conditions mediated by matrix metalloproteinases and TACE, such as tumor growth, osteoarthritis, rheumatoid arthritis and degenerative cartilage loss.
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- 2-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use
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Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- Synthesis of substituted 10,11-dihydro-5H-dibenz[b,f]azepines; key synthons in syntheses of pharmaceutically active compounds
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Substituted 10,11-dihydro-5H-dibenz[b,f]azepines are key synthons in the syntheses of a number of pharmaceutically active compounds such as imipramine, chlorimipramine, and desimipramine analogues. A facile synthesis of substituted 10,11-dihydro-5H-dibenz[b,f]azepines is described, starting out from commercially available 2-bromotoluenes or 2-nitrotoluenes. Initial α-bromination with N-bromosuccinimide and subsequent reaction with triethylphosphite afforded the corresponding benzyl phosphonic ester derivatives. After reaction with benzaldehyde derivatives, the expected Horner-Emmons reaction products were obtained. Hydrogenation gave the amino derivatives which were transformed into the corresponding formamides. Under Goldberg conditions [1], the final ring closing step was performed to give the substituted 10,11-dihydro-5H-dibenz[b,f]azepines in 46-75% yield.
- Jorgensen, Tine Krogh,Andersen, Knud Erik,Lau, Jesper,Madsen, Peter,Huusfeldt, Per Olaf
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- A Comparative Study of the Rearrangement of Some 6- and 7-Halo-substituted 3-Amino-3,4-dihydro-1-hydroxycarbostyrils in Concentrated Hydrohalic Acids
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The 6-bromo (16), 6-fluoro (17), 7-bromo (14) and 7-fluoro (15), substituted 3-amino-3,4-dihydro-1-hydroxycarbostyrils were treated with concentrated hydrochloric and hydrobromic acids under reflux conditions.The 7-halogenated N-hydroxycarbostyrils (14,15) gave the normal rearrangement products, the 6,7-dihalolactams (18-21).The 6-halogenated compounds (16,17) yielded the corresponding 6,8-dihalolactams (22-24) under the same experimental conditions, with the exception of the hydrobromic acid reaction of the 6-fluoro derivative 17 which yielded a mixture of products.Based on the comparison of the nmr spectrum of the product mixture with those of two authentic compounds, the mixture was identified as consisting of the normal rearrangenent product, the 8-bromo-6-fluorolactam (27) and the straightforward reduction product, the 6-fluorolactam (26) in ratio of about 2:1.The latter compounds were prepared by an independent method of synthesis in which 2-amino-5-fluorophenylalanine (25) was acidified to yield the yield the corresponding lactam 26, followed by bromination to afford the 8-bromo-6-fluorolactam 27.A mechanism is propopsed to interpret the experimental results of nucleophilic substitution with rearrangement and reduction which occur with the 6-fluoro compound 17 when exposed to bromide ions in strongly acidic solution.
- McCord, Tommy J.,Crawford, Charles P.,Rabon, James A.,Gage Larry D.,Winter, J. Mark,Davis, Alvie L.
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p. 401 - 406
(2007/10/02)
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