849928-34-3Relevant academic research and scientific papers
Highly Enantioselective Catalytic Addition of Grignard Reagents to N-Heterocyclic Acceptors
Guo, Yafei,Harutyunyan, Syuzanna R.
supporting information, p. 12950 - 12954 (2019/08/07)
General methods to prepare chiral N-heterocyclic molecular scaffolds are greatly sought after because of their significance in medicinal chemistry. Described here is the first general catalytic methodology to access a wide variety of chiral 2- and 4-substituted tetrahydro-quinolones, dihydro-4-pyridones, and piperidones with excellent yields and enantioselectivities, utilizing a single catalyst system.
A 1 - tert-butoxy carbonyl -2 - methyl -4 - piperidone method for the synthesis of
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, (2016/12/07)
The invention discloses a synthesis method of 1-tertbutyloxycarbonyl-2-methyl-4-piperidone. The synthesis method comprises the following steps: step one, synthesis of 1-Cbz-2-methyl-3,4-dihydro-4-piperidone; step two, synthesis of 1-Cbz-2-methyl-4-piperid
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency
Egbertson, Melissa,McGaughey, Georgia B.,Pitzenberger, Steven M.,Stauffer, Shaun R.,Coburn, Craig A.,Stachel, Shawn J.,Yang, Wenjin,Barrow, James C.,Neilson, Lou Anne,McWherter, Melody,Perlow, Debra,Fahr, Bruce,Munshi, Sanjeev,Allison, Timothy J.,Holloway, Katharine,Selnick, Harold G.,Yang, Zhiqiang,Swestock, John,Simon, Adam J.,Sankaranarayanan, Sethu,Colussi, Dennis,Tugusheva, Katherine,Lai, Ming-Tain,Pietrak, Beth,Haugabook, Shari,Jin, Lixia,Chen,Holahan, Marie,Stranieri-Michener, Maria,Cook, Jacquelynn J.,Vacca, Joseph,Graham, Samuel L.
, p. 4812 - 4819 (2015/10/28)
The IC50 of a beta-secretase (BACE-1) lead compound was improved ~200-fold from 11 μM to 55 nM through the addition of a single methyl group. Computational chemistry, small molecule NMR, and protein crystallography capabilities were used to com
ANTIBACTERIAL QUINOLINE DERIVATIVES
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Paragraph 0213; 0214, (2015/02/25)
The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a s
HEPATITIS B ANTIVIRAL AGENTS
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, (2013/07/05)
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
LACTAMS AS BETA SECRETASE INHIBITORS
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, (2013/02/28)
Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermedia
Copper-catalyzed asymmetric 1,4-addition of alkenyl alanes to N-substituted-2-3-dehydro-4-piperidones
Mueller, Daniel,Alexakis, Alexandre
supporting information; body text, p. 1842 - 1845 (2012/06/18)
Readily available vinyl alanes are used in the Cu-catalyzed asymmetric conjugate addition reaction to N-substituted-2-3-dehydro-4-piperidones. The enhanced reactivity of recently developed and easily prepared phosphine amine ligands in combination with inexpensive Cu(II)naphtenate (CuNp) allows the introduction of a great variety of alkenyl, alkyl, and aryl aluminums in high enantioselectivity.
LACTAMS AS BETA SECRETASE INHIBITORS
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Page/Page column 37-38, (2010/07/10)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis,
SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 30-31; 37-38, (2010/11/25)
The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as
Discovery of potent and selective inhibitors of 11β-HSD1 for the treatment of metabolic syndrome
Richards, Steven,Sorensen, Bryan,Jae, Hwan-soo,Winn, Marty,Chen, Yixian,Wang, Jiahong,Fung, Steven,Monzon, Katina,Frevert, Ernst U.,Jacobson, Peer,Sham, Hing,Link
, p. 6241 - 6245 (2007/10/03)
High throughput screening efforts have identified a novel class of dichloroaniline amide 11β-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4 focused on retaining the potency and selectivity profile of the lead.
