3952-66-7Relevant academic research and scientific papers
FUSED MULTI-CYCLIC SULFONE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF
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Paragraph 0784, (2014/08/07)
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
Highly chemo-, enantio-, and regioselective synthesis of α,α-disubstituted furanones by Cu-catalyzed conjugate addition
Endo, Kohei,Yakeishi, Sayuri,Takayama, Ryotaro,Shibata, Takanori
supporting information, p. 8893 - 8897 (2014/07/22)
A highly chemo-, enantio-, and regioselective synthesis of furanones bearing an α,α-disubstituted quaternary stereogenic center is reported. The Cu-catalyzed enantioselective conjugate addition of organoaluminum reagents to unsaturated ketoesters at room temperature and subsequent lactonization took place. Synthetic transformations of furanones represent facile approaches to various cyclic or acyclic compounds bearing a quaternary stereogenic center. Selective chemistry: A highly chemo-, enantio-, and regioselective synthesis of furanones bearing an α,α-disubstituted quaternary stereogenic center is reported (see scheme). Cu-catalyzed enantioselective conjugate addition of organoaluminum reagents to unsaturated ketoesters at room temperature and subsequent lactonization took place.
Oxone-mediated oxidative cleavage of β-keto esters and 1,3-diketones to α-keto esters and 1,2-diketones in aqueous medium
Stergiou, Anastasios,Bariotaki, Anna,Kalaitzakis, Dimitris,Smonou, Ioulia
, p. 7268 - 7273 (2013/08/15)
A versatile and highly efficient method for the direct synthesis of α-keto esters and 1,2-diketones has been developed. This approach utilizes the oxidative cleavage of a variety of β-keto esters and 1,3-diketones mediated by an Oxone/aluminum trichloride system. The simple one-step oxidation reaction proceeded selectively in aqueous media to afford products in high yields, short reaction times, and environmentally benign conditions.
Syntheses of heterocyclic ethenyl C-nucleosides for recognition of inverted base pairs within the DNA triple helix by stereoselective intramolecular cyclization and olefin metathesis
Rothman, Jeffrey H.
scheme or table, p. 925 - 928 (2009/06/20)
Canonical recognition of gene sequences would allow precise means for specific genetic intervention. Unfortunately, specific recognition of two of the four possible base pairs by triplex-forming oligonucleotide (TFO) as X ? T-A and Y ? C-G within a triple
METHOD FOR GRIGNARD TYPE REACTIONS IN MICROREACTORS
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Page/Page column 16-17; 19, (2008/06/13)
The present invention relates to a process for Grignard type reactions comprising mixing at least two fluids in a microreactor having at least two injection points.
PROCESS FOR PRODUCING ALPHA-OXOCARBONYL COMPOUND
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Page/Page column 6, (2008/06/13)
A process by which an α-oxocarbonyl compound useful as an intermediate for pharmaceuticals/agricultural chemicals can be industrially advantageously and efficiently produced in a high yield. The process, which is for producing an α-oxocarbonyl compound represented by the general formula (I) wherein R1 and R2 are as defined in the description, comprises oxidizing an α-hydroxycarbonyl compound represented by the general formula (II) , with oxygen or air in the presence of a carboxylic acid and at least one vanadium compound selected from divanadium pentaoxide, divanadium trioxide, divanadium tetraoxide, ammonium metavanadate, sodium metavanadate, potassium metavanadate, triethoxyoxovanadium, tripropoxyoxovanadium, triisopropoxyoxovanadium, vanadium oxobis(acetylacetonate) and vanadium tris(acetylacetonate).
PROCESS FOR PREPARATION OF 2-OXOCARBOXYLIC ACID ESTERS
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Page 5-6, (2008/06/13)
A process for the preparation of 2-oxocarboxylic acid esters represented by the following general formula (I), comprising by oxidizing a 2-hydroxycarboxylic acid ester represented by the following general formula (II) in the presence of a nitroxyl radical represented by the following general formula (III), a hypochlorite, a metal bromide and water with the pH of the reaction system being kept within the range of 5 to 7: (I) (II) (III) wherein R1 and R2 are each independently an alkyl group, an alkenyl group, an alkynyl group, an aryl group or an aralkyl group, which each may be substituted with substituents; and R3 is a hydrogen atom, an alkoxyl group, an aralkyloxy group, an acyloxy group or a hydroxyl group.
2-oxo-1-pyrrolidine derivatives, process for preparing them and their uses
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, (2008/06/13)
The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing α-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particularly the invention concerns novel intermediates and their use in methods for the preparation of S-α-ethyl-2-oxo-1-pyrrolidine acetamide.
A selective method for the preparation of aliphatic methyl esters in the presence of aromatic carboxylic acids
Rodriguez,Nomen,Spur,Godfroid
, p. 8563 - 8566 (2007/10/03)
2,2-Dimethoxypropane, methanol and a catalytic amount of HCl selectively esterify aliphatic carboxylic acids, in the presence of aromatic carboxylic acids, at room temperature and in high yields.
Conversion of α-keto esters into β,β-difluoro-α-keto esters and corresponding acids: A simple route to a novel class of serine protease inhibitors
Parisi,Gattuso,Notti,Raymo,Abeles
, p. 5174 - 5179 (2007/10/02)
The preparation of a series of β,β-difluoro-α-keto esters and corresponding acids RCF2COCO2R' (R=Me, Et, i-Pr, Bn, and Ph; R'=Et and H), designed as potential inhibitors of serine proteases, is described. The standard procedure developed consists in the initial formation of an α,α- difluoro ester from an α-keto ester, followed by a simple four-step sequence involving the synthesis of hemiacetal, cyanohydrin, and α-hydroxy ester difluorinated intermediates. This method provides an easy route to β,β- difluoro-α-keto esters and corresponding acids, via 'formal' insertion of a difluoromethylene group between the R substituent and the α-carbonyl group of a generic α-keto ester.
