Abstract: The invention includes a method of treating a solid acid catalyst. After exposing the catalyst to a mixture containing a sugar alcohol, the catalyst is washed with an organic solvent and is then exposed to a second reaction mixture. The invention includes a process for production of anhydrosugar alcohol. A solid acid catalyst is provided to convert sugar alcohol in a first sample to an anhydrosugar alcohol. The catalyst is then washed with an organic solvent and is subsequently utilized to expose a second sample. The invention includes a method for selective production of an anhydrosugar. A solid acid catalyst is provided within a reactor and anhydrosugar alcohol is formed by flowing a starting sugar alcohol into the reactor. The acid catalyst is then exposed to an organic solvent which allows a greater amount of additional anhydrosugar to be produced than would occur without exposing the acid catalyst to the organic solvent.

Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones as novel, efficient sulfur-transfer reagents is disclosed. The sulfur transfer from these reagents to compounds containing P(III) atom, triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite, was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.

Abstract: The invention provides methods of purifying rebaudioside A from a mixture comprising glycosides of the plant Stevia rebaudiana. The methods of the invention are useful for preparing highly pure rebaudioside A compositions from crude Stevia starting compositions that are typically considerably lower in rebaudioside A concentration. The highly pure rebaudioside A compositions are useful as non-caloric sweeteners in edible or chewable compositions such as food, beverages, medicine, candy, chewing gum, and the like.

Abstract: The present invention pertains to methods of extracting cardiac glycosides from cardiac glycoside containing plant material, such as Nerium oleander, through use of aloe. It further provides for compositions resulting from such extractions, pharmaceutical compositions, cosmetic compositions, and methods of treating skin conditions.

Abstract: Spinetoram is selectively produced in excellent yields by hydrogenating a mixture of 3?-O-ethyl spinosyn J and 3?-O-ethyl spinosyn L in a water miscible organic solvent using hydrogen gas and a heterogeneous catalyst.

Abstract: Disclosed are methods for preparing 2-alkynyladenosine derivatives of formula A: or a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate, acid salt hydrate or isomorphic crystalline form thereof, the method comprising the step of: contacting 2-iodoadenosine-5?-N-ethyluronamide with a compound of formula B: wherein Z is —C(?O)OR or —CH2C(?O)R, where R is a C1 to C5 alkyl, preferably The methods are useful for preparing 2-alkynyladenosine derivatives that are, in certain embodiments, adenosine receptor agonists.

Abstract: Improved methods to prepare aqueous extracts of gallic acid esters including 1-O-galloyl-?-D-glucose (?-glucogallin) and other mucic acid gallates from the fruits of Emblica officinalis, wherein enrichment of gallic acid esters is achieved by Supercritical Fluid Extraction (SCFE) procedure, are disclosed. The use of such standardized extracts of gallic acid esters (greater than 40% w/w of gallic acid esters) in the manufacture of medicaments with diverse health benefits, is also disclosed.

Abstract: The invention includes methods of producing dianhydrosugars. A polyol is reacted in the presence of a first catalyst to form a monocyclic sugar. The monocyclic sugar is transferred to a second reactor where it is converted to a dianhydrosugar alcohol in the presence of a second catalyst. The invention includes a process of forming isosorbide. An initial reaction is conducted at a first temperature in the presence of a solid acid catalyst. The initial reaction involves reacting sorbitol to produce 1,4-sorbitan, 3,6-sorbitan, 2,5-mannitan and 2,5-iditan. Utilizing a second temperature, the 1,4-sorbitan and 3,6-sorbitan are converted to isosorbide. The invention includes a method of purifying isosorbide from a mixture containing isosorbide and at least one additional component. A first distillation removes a first portion of the isosorbide from the mixture. A second distillation is then conducted at a higher temperature to remove a second portion of isosorbide from the mixture.

Abstract: The present invention provides luminescent metal ion complexes for use in a wide range of biological and chemical studies. The luminescent metal ion complexes of the invention comprise a metal ion chelating component covalently bound to a carrier molecule. Also provided are methods of making and using the luminescent metal ion complexes.

Abstract: The invention includes methods for producing dianhydrosugar alcohol by providing an acid catalyst within a reactor and passing a starting material through the reactor at a first temperature. At least a portion of the staring material is converted to a monoanhydrosugar isomer during the passing through the column. The monoanhydrosugar is subjected to a second temperature which is greater than the first to produce a dianhydrosugar. The invention includes a method of producing isosorbide. An initial feed stream containing sorbitol is fed into a continuous reactor containing an acid catalyst at a temperature of less than 120° C. The residence time for the reactor is less than or equal to about 30 minutes. Sorbitol converted to 1,4-sorbitan in the continuous reactor is subsequently provided to a second reactor and is dehydrated at a temperature of at least 120° C. to produce isosorbide.

Abstract: The present invention provides a method for producing sucralose from a feed stream resulting from the chlorination of a sucrose-6-acylate in a reaction vehicle. The feed stream includes a sucralose-6-acylate, the reaction vehicle, water, and salts. The salts include one or more selected from the group consisting of alkali metal chlorides, alkaline earth metal chlorides and ammonium chloride. The method includes: (i) deacylation of the sucralose-6-acylate by treatment with a base to afford a product stream comprising sucralose; (ii) partial removal of water and, optionally, reaction vehicle from the product stream of (i) in order to cause precipitation of the salts from the product stream; (iii) removal of the precipitated salts from the product stream of (ii); and (iv) isolation of sucralose from the product stream of (iii).

Abstract: The synthesis of the naturally occurring kaempferol glycoside SLO1O1-1, as well as analogs thereof, has been accomplished, as has its biochemical evaluation. SLO1O1-1 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. The synthetic scheme of the invention verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation.

Abstract: The present invention provides a method for producing sucralose from a feed stream including a sucrose-6-acylate in a reaction vehicle.

Abstract: Sulfoquinovosylacyl propanediol compounds represented by formula (I): wherein R1 is an acyl residue of a fatty acid, Y is a number of 1, 2 or 3, and M represents a cation having a positive charge equal to Y and pharmaceutically acceptable salts thereof are effective for treating tumors.

Abstract: The present invention provides a method of preparing a glycoside of a mono- or diacylglycerol product from a plant material. The method comprises the steps of: (i) optionally milling the plant material, (ii) extracting the optionally milled plant material with a first aqueous extraction solution obtaining a first liquid phase and a first solid phase, (iii) separating the liquid phase from the solid phase to obtain a glycoside of mono- or diacylglycerol product, (iv) extracting the solid phase from step (iii) with a second extraction solution obtaining a second liquid phase and a second phase, and (v) separating the second liquid phase from the second solid phase to obtain a second and a third glycoside of mono- or diacylglycerol product, wherein the second extraction solution further comprises a cell wall degrading enzyme or a mixture of cell wall degrading enzymes.

Abstract: A process of preparing an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate, which is useful as an intermediate in the preparation of a beta nucleoside, such as gemcitabine, an anti-tumor agent. A beta-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate is heated and converted to an alpha-2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate in the absence of an effective amount of a sulfonate salt to facilitate the conversion. In addition, an anomeric mixture of an alpha-anomer and a beta-anomer of 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate can be dissolved in a mixture of water and a solvent and heated to produce a lactol, which may be further converted to an alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofunanosyl sulfonate.

Abstract: The present invention provides compounds and methods of using them for preparing bicyclic nucleosides. The bicyclic nucleosides are useful for preparing chemically modified oligomeric compounds. Oligomeric compounds comprising these bicyclic nucleosides have enhanced properties such as increased nuclease resistance.

Abstract: A sensor for the detection or measurement of a carbohydrate analyte in fluid comprises components of a competitive binding assay the readout of which is a detectable or measurable optical signal retained by a material that permits diffusion of the analyte but not the assay components, the assay components comprising: a carbohydrate binding molecule labelled with one of a proximity based signal generating/modulating moiety pair; and a carbohydrate analogue capable of competing with the analyte for binding to the carbohydrate binding molecule, the carbohydrate analogue being a flexible water-soluble polymer comprising: polymerized or co-polymerised residues of monomer units, the monomer unit residues bearing pendant carbohydrate or carbohydrate mimetic moieties and pendant moieties which are the other of the proximity based signal generating/modulating moiety pair.

Abstract: Compounds of 5-thioxylopyranose, preferably derivatives of the 5-thioxilopyranose type, a method for preparing such compounds, and the use of such compounds as an active ingredient in pharmaceutical compositions which are useful, in particular, for treating or inhibiting thrombosis or heart failure or thromboembolic disease states.

Abstract: The present invention relates to a compound having a cyclodextrin skeleton wherein a hydrogen atom at the C-6 position in at least one of the sugar moieties has been substituted with a cyano group thereby forming a cyanohydrin-type group. The compounds are found to be excellent catalysts, e.g. for the hydrolysis of aryl glycosides. Accordingly, the compounds of the invention are useful as medicaments, in particular for the treatment of poisoning and drug abuse. The compounds, optionally immobilized to a solid phase material, are useful to reduce the content of harmful substances, e.g. metabolites of fungi, insects, etc., from compositions such as foodstuff.

Abstract: The present invention relates to pharmaceutically active oligosaccharide conjugates having the formula: (X—Ym)n—S, wherein component X is a pharmaceutically active compound, Y is a bifunctional linker, and S is an oligosaccharide consisting of 1 to 20 saccharide units, n is equal or less than the number of the saccharide units in the oligosaccharide S, and m is, independent of n, 0 or 1. In addition, the present invention is directed to a process of preparing compounds of the present invention, comprising the step of coupling components X and S directly or indirectly by means of a bifunctional linker group. Furthermore, the present invention relates to the use of said pharmaceutically active oligosaccharide conjugates as a medicament as well as to pharmaceutical compositions, freeze-dried pharmaceutical compositions, and a kit, all of which comprise at least one of said pharmaceutically active oligosaccharide conjugates.

Abstract: The present invention relates to methods of preparing anthocyanins, and methods of preparing precursors of anthocyanins. The methods utilise a coupling reaction between a sugar and a suitable electrophilic precursor to form Eastern half intermediates that are then reacted with Western half intermediates to form the target anthocyanins. Some Eastern half intermediates and electrophilic precursors also form part of the invention.

Abstract: The invention relates to a crystalline form of 1?-(1-methylethyl)-4?-[(2-fluoro-4-methoxyphenyl)methyl]-5?-methyl-1H-pyrazol-3?-O-?-D-glucopyranoside, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.

Abstract: A method for preparing hexose derivatives comprises the steps of providing a silylated hexose, treating the silylated hexose with a first carbonyl compound in the presence of a catalyst to form an ketalized hexose, treating the ketalized hexose with a second carbonyl compound followed by treating with a first reductant to form an etherized hexose, and converting the etherized hexose into a target hexose derivative, which can be 2-alcohol hexose, 3-alcohol hexose, 4-alcohol hexose, or a 6-alcohol hexose.

Abstract: The present invention relates to a process for the production of cross-linked hyaluronic acid (HA) derivatives, in particular multiple, e.g. double cross-linked hyaluronic acid derivatives. The invention also provides novel cross-linked HA derivatives, products containing them and their uses in medical and pharmaceutical and cosmetic applications.

Abstract: The present invention is a method of preparing affinity ligands, which method comprises to provide a cyclic scaffold comprising a thiol group, a carbonyl group and an amine group; to derivatize the amine group of said scaffold with an electrophile that carries either a functionality capable of affinity interaction or a functionality capable of a second interaction with a target molecule; and to open up the derivatized scaffold and add an amine that carries either a functionality capable of a second interaction or a functionality capable of affinity interaction with a target molecule. The method provides provide affinity ligands, which are capable of affinity interaction as well as a second kind of interaction.

Abstract: 3-O-?-D-Glucopyranosyl-4-methylergost-7-en-3-ol or a composition containing 0.001% by mass or more of the aforementioned compound, which is an extract of a plant of the family Liliaceae containing the compound or a fraction thereof, is used as an active ingredient of a hyperglycemia improving agent.

Abstract: The invention relates to a method for producing drug extracts that contain hydroxystilbene from a vegetable drug and to the use of various agents for pharmaceutical and non-pharmaceutical purposes.

Abstract: To provide a method for efficiently and industrially deuterating the benzyl position of a —O-benzyl group formed by introducing a benzyl group, a benzyloxymethyl group and the like as a protecting group. The deuteration method for the benzyl position of a —O-benzyl group of a compound having the —O-benzyl group which may have a substituent, comprising reacting the compound with a heavy hydrogen source in the coexistence of a palladium/carbon-ethylenediamine complex and hydrogen.

Abstract: The invention relates to novel 5-thioxylose compounds, preferably derivatives of the 5-thioxylopyranose type, to the method for their preparation and to their use as active principles of drugs intended especially for the treatment or prevention of thromboses or cardiac insufficiency.

Abstract: A process for preparing a sucralose-6-ester, a key intermediate to sucralose. The process contains (a) creating a heterogeneous mixture comprising a first phase comprising a sucrose-6-ester and a second phase comprising a chlorinating reagent; and (b) reacting the sucrose-6-ester with the chlorinating reagent, to prepare a sucralose-6-ester. In addition, processes for preparing sucralose from sucrose-6-esters are provided.

Abstract: A process for modifying an organic natural substance by exchange reactions is characterised in that the natural substance to be modified is heated in the liquid phase as an aerosol in a gas stream, with the exclusion of air, along a conveyance path and, after reaching a temperature dependent on the bond energy of the molecules and/or molecular groups to be exchanged, is removed from the conveyance path to supply to the natural substance to be modified the materials required for the exchange reaction under the respectively required reaction conditions, and in that the reaction product is then supplied to the conveyance path in the circuit and heated to an elevated reaction temperature for carrying out the exchange reactions before the reaction product is withdrawn from the conveyance path and condensed to obtain the modified natural substance.

Abstract: A process is provided for the preparation of anhydrosugar alcohols. The process involves heating a sugar alcohol or a monoanhydrosugar alcohol starting material in the presence of an acid catalyst, and subsequent purification of the anhydrosugar alcohol. In some embodiments of the present invention, film evaporators are used in distillation and purification of the anhydrosugar alcohols. Anhydrosugar alcohols of very high purity are achieved in the practice of the present invention. In some embodiments of the present invention, very high purities of the anhydrosugar alcohols are achieved without the use of organic solvents.

Abstract: The present invention relates to a one-step process for the selective O-acylation of the hydroxy groups of a nucleoside under basic conditions utilizing DMAP and a carboxylic acid anhydride in aqueous heterogenous solvent mixture.

Abstract: The present invention relates to the chemical synthesis of solanum glycosides, in particular to the synthesis of solasonine as well as to novel ?-monosaccharide intermediate compounds, of Formula (2), where R1 is a benzylidene, 4-nitrobenzylidene or 4-methoxybenzylidine group, and each R2 independently is a benzoyl, acetyl or pivaloyl group:

Abstract: The present invention is directed to synthetic molecules having biological activity similar to PIM (acyl glycerol phosphatidylinositol manno-oligosacccharide) activity, for use in the treatment and prevention of inflammatory or immune cell mediated diseases or disorders.

Abstract: The present invention relates to novel nucleoside derivatives of general formula (I) wherein R1=H, halogen, NO2, CN, OCH3, an alkyl, alkoxy or alkoxyalkyl residue having 1 to 4 C atoms, preferably a methyl, ethyl, propyl or butyl residue or an optionally substituted aryl residue or aliphatic acyl residue having 2 to 5 atoms, R2 to R7=H, NO2, CN, OCH3, a branched or unbranched alkyl, alkoxy or alkoxyalkyl residue having 1 to 5 C atoms or an optionally substituted aryl residue or an aliphatic acyl residue having 2 to 5 atoms, X is the group C?O or C?S, Y?S, O, NR?, C(R?)2, wherein R? is H, or a branched or unbranched alkyl residue having 1 to 5 C atoms or an optionally substituted aryl residue, Z=SO2, OCO, OCS, SCS, and N is a nucleotide.

Abstract: There is provided a method for the production of sucralose from a feed stream resulting from the chlorination of a sucrose-6-acylate in a reaction vehicle, said feed stream comprising a sucralose-6-acylate, the reaction vehicle, and by-products including high molecular weight coloured material, said method comprising: deacylation of the sucralose-6-acylate by treatment with a base to afford sucralose, and, before or after said deacylation, removal of the reaction vehicle and isolation of the sucralose characterised in that immediately before the removal of the reaction vehicle, the reaction stream is subjected to a precipitation step comprising treatment with a metal or ammonium hydroxide and carbon dioxide to form a precipitate of the corresponding metal or ammonium carbonate in which at least a portion of said high molecular weight coloured material is trapped, followed by separation of said precipitate.

Abstract: A solid phase synthetic method is disclosed in which the usual solid phase synthetic steps are carried out and the spent solid phase support is reacted to form a volatilizable compound upon cleavage of the reaction product from the solid phase support. The cleaved product is then separated from the volatile compound by volatilization of that compound. Exemplary solid supports that form a volatilizable compound are also disclosed.

Abstract: Compounds and methods are provided for obtaining oligosaccharide mimics. More specifically, compounds and methods are described wherein oligosaccharide mimics are obtained by incorporating or substituting in a cyclohexane derivative.

Abstract: This invention describes a process for producing a fraction enriched with jujubogenin and psudojujubogenin lycosides from Bacopa species, wherein the total Bacopa saponin concentration is up to 100% when estimated by HPLC method of analysis. The present invention also describes the processes for the enrichment of new compositions and individual saponin compounds from Bacopa munnieri to more than 95% purity. It further describes an analytical HPLC method for the estimation of total Bacopa saponin fraction and its use in therapeutic applications. This invention also includes two Bacopa saponin 3-O-[?-D-glucopyranosyl-(1 3)-?-D-glucopyranosyl] jujubogenin and 3-O-[?-D-glucopyranosyl-(1 3)-?-D-glucopyranosyl] pseudojujubogenin herein referred to as bacopaside N1 of general formula (1) and bacopaside N2 of general formula (2) respectively.

Abstract: The present invention relates to glucopyranosyloxy-pyrazoles of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on sodium-dependent glucose cotransporter SGLT, the use thereof for the treatment of diseases, particularly metabolic disorders such as diabetes, and the preparation thereof.

Abstract: The invention relates to novel derivatives of morphine-6-glucuronide, the preparation method thereof and the uses of same in therapy, for example, as analgesics.

Abstract: [Object] It is intended to provide a crystalline maltitol powder less prone to consolidation, which is free from the formation of a lump during delivery or storage thereof, does not require pulverization or re-classification in use, is easy to handle in transfer, package opening, addition or mixing to another food material, and so on, and allows for automated transportation and so on. [Means for Solving the Object] The crystalline maltitol powder less prone to consolidation is obtained by charging crystalline or powdery maltitol into a shelf type dryer, a tunnel-type dryer, a cylindrical container, or the like and subjecting the equipment or container to a treatment wherein an air having a temperature of 30 to 33° C. and a relative humidity of 5% is allowed to flow into the equipment or container from one side thereof and withdrawn out of the other side thereof at a space velocity of 11 to 12 for consecutive 24 hours.

Abstract: Compounds having the formula (I): wherein A represents a group such as a cyclic group, R1 and R2 represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof have superior activity and stability, and are useful for the treatment and/or prevention of diabetes mellitus, or the like.

Abstract: Herein described is a process for the preparation of 1-chloro-3,5-di-O-acyl-2-de-oxy-L-ribofuranoside derivatives of general formula (I) useful as intermediates in processes for preparing nucleotides of the L series having antiviral activity

Abstract: A process is provided for the selective and convenient production of a glycerol glycoside, which has been glycosidated at the 1-hydroxyl group of glycerol and is useful as a glyceroglycolipid precursor, humectant or the like. A glycerol carbonate glycoside represented by the following formula (1): wherein G represents a monosaccharide residue, and n stands for an integer of from 1 to 3; a process for producing the glycerol carbonate glycoside of formula (1) by reacting a saccharide with glycerol-1,2-carbonate in the presence of an acid; and a process for producing a glycerol glycoside which is represented by the following formula (2): wherein G and n have the same meanings as defined above, by deprotecting the glycerol carbonate glycoside represented by formula (1).

Abstract: The products of the invention are polymers of carboxylated alkylpolyglycosides. The products are very mild surfactants that are useful in personal care applications.

Abstract: Processes for the production of Hoodia plant extracts with a high content of steroidal glycosides and for minimizing heavy metal and/or polyaromatic hydrocarbon content in Hoodia extracts.

Abstract: The subject-matter of the invention is a process for the stereoselective preparation of a compound of general formula I by stereoselective displacement by a nitrogenous nucleophilic compound of the activated alcohol functional group present at this 4? position in a corresponding derivative of formula II.