Abstract: Described is a catalytic process for converting biomass to furan derivatives (e.g., furfural, furfuryl alcohol, etc.) using a biphasic reactor containing a reactive aqueous phase and an organic extracting phase containing an alkylphenol. The process provides a cost-effective route for producing furfural, furfuryl alcohol, levulinic acid hydroxymethylfurfural, ?-valerolactone, and the like. The products formed are useful as value-added intermediates to produce polymers, as precursors to diesel fuel, and as fuel additives.

Abstract: A method for preparing ?-keto acids, especially ?-ketomethionine, and/or derivatives thereof, whereby an aldehyde is reacted with thiols to give a corresponding dithioacetal, the dithioacetal formed, is reacted with an electrophile in the presence of a strong base, and the resulting ?,?-(dithio)carboxylic acid is solvolyzed with acid-catalysis to release thiol and give the ?-keto acid or a derivative thereof. Umpolung of aliphatic or aromatic aldehydes is effected by reaction with thiols.

Abstract: The present invention relates to novel alkoxy enones and enamino ketones, and to a novel process for preparation thereof. Alkoxy enones and enamino ketones are valuable intermediates for preparation of pyrazoles and anthranilamides, which can be used as insecticides.

Abstract: A process for preparing alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrates (VI) where R is methyl or ethyl, from crude reaction mixtures of alkyl 4,4-difluoroacetoacetates (I) by a) reacting ?where M is a sodium or potassium ion, and ?without additional solvent to form an enolate (V) b) releasing the corresponding alkyl 4,4-difluoroacetoacetate (I) from the enolate (V) by means of acid, c) removing the salt formed from cation M and acid anion as a solid and d) converting (I), without isolation from the crude reaction mixture, to the alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrate (VI), and the use of (VI) for preparing 1-methyl-3-difluoromethyl-pyrazol-3-ylcarboxyates VII

Abstract: The present invention is directed to the labeled compounds, wherein C* is each either 13C and 12C where at least one C* is 13C, each hydrogen of the methylene group is hydrogen or deuterium, the methyl group includes either zero or three deuterium atoms, Q is sulfide, sulfinyl, or sulfone, Z is an aryl group such as 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, or a phenyl group wherein R1, R2, R3, R4 and R5 are each independently either hydrogen, a C1-C4 lower alkyl, a halogen, and an amino group such as NH2, NHR and NRR? where R and R? are each independently either a C1-C4 lower alkyl, a phenyl, and an alkoxy group, and the methyl group can include either zero or three deuterium atoms.

Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.

Abstract: A trifluoromethylthiophenium derivative salt useful as synthetic intermediates for pharmaceuticals and agrochemicals, a method for producing the same, and a method for producing trifluoromethyl-containing compounds using the same are provided. An S-(trifluoromethyl)-benzo[b]thiophenium derivative salt is represented by the following general formula (1): wherein R1, R2, R3, and R4 are each independently a hydrogen atom, a methyl group, an ethyl group, a linear, branched, or cyclic alkyl group having 3 to 10 carbon atoms, a methoxy group, an ethoxy group, a linear, branched, or cyclic alkyloxy group having 3 to 10 carbon atoms, a fluorine atom, a chlorine atom, a bromine atom, a nitro group, or a cyano group, R5 is a methyl group, an ethyl group, a linear, branched, or cyclic alkyl group having 3 to 10 carbon atoms, a phenyl group, or a substituted phenyl group, and X? represents an anion.

Abstract: Disclosed is a method of preparing a petroleum-alternative bio fuel material such as 5-hydroxymethyl-2-furfural (HMF), 5-alkoxymethyl-2-furfural, levulinic acid alkil ester, etc. through a single process without saccharification, using a catalyst conversion reaction, from galactan that can be massively supplied at low costs and extracted from macroalgae of marine reusable resources. Thus, the macroalgae of the marine biomass resources is used so that a carbon source can be more easily extracted than that of a lignocellulosic biomass resource without a problem of having an effect on grain price like a crop-based biomass.

Abstract: Disclosed is a method for preparing 7-halo-2-oxoheptylate, an intermediate of cilastatin. The main steps are as follows: A. Addition reaction, in which 6-halo-hexanal is reacted with a cyanide to obtain 7-halo-?-hydroxyl-heptonitrile; B. Hydrolysis reaction, in which 7-halo-?-hydroxyl-heptonitrile is converted to 7-halo-?-hydroxyl-heptylic acid; C. Esterification reaction, in which 7-halo-?-hydroxyl-heptylic acid is converted to 7-halo-?-hydroxyl-heptylate; and D. Oxidation reaction, in which 7-halo-?-hydroxyl-heptylate is converted to 7-halo-2-oxoheptylate. 7-halo-?-hydroxyl-heptylic acid or ester thereof, which is a new intermediate for synthesizing 7-halo-2-oxoheptylate or cilastatin, and a method for synthesizing cilastatin are also disclosed. The methods of the invention are suitable for commercial production because of their simple process and mild reaction condition.

Abstract: Composition of esters of fluorosubstituted alcanoic acids, comprising or consisting essentially of a compound of a formula selected from the group consisting of: RCFClC(OAc)?CHC(O)OR1 (II); RCFHC(O)CH2C(O)OR1 (IV); RCFHC(OAc)?CHC(O)OR1 (V); and RCFHCH(OAc)CH2C(O)OR1 (VI); or of compounds of formula (I) RCFClC(O)CH2C(O)OR1 and of formula (II); of compounds of formulae (IV) and (V); or of compounds of formulae (IV) and (VI); wherein R is C2F5, CF3 or F and R1 is an alkyl group with from 1 to 4 carbon atoms, an alkyl group with from 1 to 4 carbon atoms substituted by 1 or more fluorine atoms. A process for the reduction of the compound of formula (I) and/or formula (II), and compositions resulting from such reduction. A process for the separation of the compound of formula (I) from the compound of formula (II) comprising subjecting a composition comprising such compounds to a distillation operation.

Abstract: The invention relates to a process for preparing alkyl dihaloacetoacetates of the formula (I) by reacting ?,?-dihaloamines of the formula (III) with acetic esters of the formula (II) in the presence of bases.

Abstract: A photosensitive compound whose size is smaller than conventional polymer for photoresist, and which has well-defined (uniform) structure, and a photoresist composition including the same are disclosed. The photosensitive compound represented by the following formula. Also, the present invention provides a photoresist composition comprising 1 to 85 wt % (weight %) of the photosensitive compound; 0.05 to 15 weight parts of a photo-acid generator with respect to 100 weight parts of the photosensitive compound; and 10 to 5000 weight parts of an organic solvent. In the formula, n is 0 or 1, x is 1, 2, 3, 4 or 5, y is 2, 3, 4, 5 or 6, z is 0, 1, 2, 3 or 4, R, R? and R? are independently hydrocarbon group of 1 to 30 carbon atoms, preferably 2 to 20 carbon atoms, and R?? is a hydrogen atom or hydrocarbon group of 1 to 30 carbon atoms, preferably 2 to 20 carbon atoms.

Abstract: A method for efficiently producing 4-(hydroxymethylphosphinyl)-2-oxobutanoic acid, useful as a production intermediate of herbicide L-AMPB. The method comprises using a compound represented by the below formula (4): (4) where R1 represents a C1-4 alkyl group, arylmethyl group, or substituted arylmethyl group.

Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and/or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A, e.g. 2A13 and 2A6, and CYP2B6.

Abstract: The invention relates to a process in which a compound R1COOR3 (I) is made by a transesterification reaction of an ester compound R1COOR2 (II) with an alcohol R3OH (III) in the presence of a transesterification catalyst, wherein R1 is H or C1-4 alkyl or CH2?CR4—; R2 is C1-4 alkyl; R3 is selected from the group consisting of alkyl having at least 4 carbon atoms, cycloalkyl having at least 5 carbon atoms, aryl, aralkyl, alkaryl and amino alkyl; and R4 is —H or —C1-4 alkyl, wherein alcohol R2OH (IV) is formed as a byproduct and in which said byproduct (IV) is removed by distillation in the presence of an entrainer, in which the entrainer is a compound that suppresses the formation of an azeotrope between compound (II) and byproduct (IV). The process can be useful in the preparation of esters such as dimethyl amino ethyl(meth)acrylate. The invention also provides a method of separating alcohols and esters.

Abstract: The present invention provides for compounds of Formulas I-III, and salts thereof, wherein n, m, R1, R2, R3, and R4 have any of the values defined there for in the specification. The compounds of formula I may be used in the synthesis of oligonucleotides such as compounds of formula II (bearing a 3?-thiol) or formula III (bearing a 3?-disulfide).

Abstract: A new process is described for the direct synthesis of esters of levulinic acid starting from biomasses containing one or more polysaccharides and from aliphatic alcohols, in the presence of a suitable organic acid catalyst. In particular, the biomasses can be lignin-cellulose biomasses. The esters thus obtained can be used as oxygenated components in the formulation of fuels for motor vehicles, with the aim of reducing the particulate emissions.

Abstract: Novel pyruvate derivatives exhibiting outstanding neuroprotective effect, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions for prevention and treatment of brain disease including them as effective ingredient are provided.

Abstract: A substituted cyclopentanone represented by the following formula (2): (wherein R3 and R4 represent a substituent having 1 to 8 carbon atoms, may be the same as R1 and R2, respectively, and may be the same as each other) can be produced by hydrogenating the double bond in a compound represented by the following formula (1): (wherein R1 and R2 represent a substituent having 1 to 8 carbon atoms) in the presence of a transition metal catalyst by using a carboxylic acid or a specific concentration of a carboxylic acid ester as a solvent. This process can produce a substituted cyclopentanone which is useful as a jasmine fragrance, an intermediate thereof or the like, in a simple and inexpensive manner at a high cis-isomer ratio.

Abstract: The present invention relates to novel alkoxy enones and enamino ketones, and to a novel process for preparation thereof. Alkoxy enones and enamino ketones are valuable intermediates for preparation of pyrazoles and anthranilamides, which can be used as insecticides.

Abstract: Process for purifying an ?-keto ester by removing secondary and tertiary alcohols from the ?-keto ester. In a first step, the ?-keto ester to be purified is treated with a carboxylic anhydride and an acid, which is essentially insoluble under the filtration conditions, to esterify the secondary and tertiary alcohols. Subsequent filtration to remove the acid followed by distillation affords the desired purified ?-keto ester.

Abstract: The present invention relates to a novel method for the preparation of racemic pregabalin (1) or a single enantiomer thereof, (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid (2).

Abstract: A process for producing levulinic acid and its esters from biomass is disclosed comprising: (i) feed preparation module characterized by subjecting biomass to a high-temperature refining treatment; (ii) hydrolysis reaction module that facilitates the hydrolysis of biomass to its respective sugars and their subsequent transformation to levulinic acid, formic acid, furfural, and char as well as facilitates the separation of lignin-based char by-product; (iii) product separation and recovery module utilizing a solvent extraction technique such as using furfural by-product as extracting solvent; and (iv) optionally, conversion of levulinic acid to levulinate ester. When desired, the disclosed process may be integrated into existing pulp mills.

Abstract: Disclosed herein are thiocolchicine derivatives suitable for use as muscle relaxants, methods of making the derivatives, and compositions comprising the derivatives.

Abstract: The present invention pertains to substances of the formula (I) wherein X is O or S; and R1-R4 are defined in the claims as inhibitors of glyoxalase I and/or II, pharmaceutical compositions comprising one or more compounds according to formula (I) and the use of one or more compounds according to formula (I) for the treatment of diseases associated with increased glycolytic metabolism. In one embodiment, the disease is a bacterial infection.

Abstract: Isotopically labeled alpha-keto acids and esters are disclosed herein. Also disclosed are methods of synthesizing isotopically labeled alpha-keto acids and esters.

Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of substantially pure Lercanidipine intermediate, 1,1,N-trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl acetoacetate. The intermediate is useful for preparing Lercanidipine, or a pharmaceutically acceptable salt thereof, in high yield and purity. The present invention further provides a novel crystalline form of Lercanidipine hydrochloride and a process for its preparation. The present invention also provides a process for the preparation of amorphous form of Lercanidipine hydrochloride.

Abstract: The present invention refers to new derivatives of the penta-1,4-dien-3-ones, as well as their processes of preparation. These compounds present strong antitumoral activity and promising antiparasitic action, behaving as almost atoxic by laboratory assays and also by hystopathologic studies. The present invention refers also to a pharmaceutical composition including the referred compounds, method of treatment for cancer and parasitic diseases.

Abstract: A 2-formylacetic ester derivative represented by the general formula (5) is provided: where R4 represents an alkyl group having 2 to 6 carbon atoms; R5 represents an alkyl group having 1 to 10 carbon atoms; and X represents H, Li, Na or K.

Abstract: A process for the preparation of a compound of Formula (1) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(?NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula (I). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, an aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ?O.

Abstract: The present invention relates to a three-step method for the preparation of alkyl esters of 4,4-difluoroacetoacetic acid in which in the first step alkyl esters of 4-chloro-4,4-difluoroacetic acid are reacted with trialkylphosphites of formula (III) P(OR1)3??(III) in which R1 stands for C1-C4-alkyl, whereby the residues R1 can in each case be the same or different, to form alkyl phosphonates of formula (IV) which in the next step are reacted with an amine of formula (V), in which R2 and R3 independent of each other stand for hydrogen or C1-C4-alkyl or together form —CH2—CH2—O—CH2—CH2—, to form enamines of formula (VI), in which R2 and R3 have the meanings described above, which in the third step are hydrolyzed in the presence of an acid.

Abstract: The present invention relates to intermediates of rosuvastatin and processes for the production thereof.

Abstract: A method of providing a fragrant odour to an application, comprising the addition thereto of at least one compound of the formula (I) wherein X and Y are independently selected from the group consisting of —CR1R2R3, —NR4R5 and —OR6, wherein R1 to R5 are selected from H and essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom, and R6 is selected from essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom; and A is an essentially hydrocarbon moiety that optionally comprises at least one oxygen, sulphur, nitrogen or silicon atom, with the proviso that the compound A-CHO is a fragrant aldehyde. The use of these compounds in laundry, household and personal care products confers a long-lasting freshness.

Abstract: The present invention comprises a novel process for the preparation of a chiral compound of formula (I) wherein R1 is hydroxyl or a group which activates the carboxyl and R2 is alkyl optionally substituted by halogen or benzyl, its preparation, its application in the synthesis of chiral 2-bromomethyl-2-ethylhexanoic acid and novel intermediates.

Abstract: Ester prodrugs of phorbol compounds for the treatment of viral infections, neoplastic diseases, inflammatory reactions, and use as analgesics, wherein the phorbol compounds are derivatized with a -x-o-c(o)-R? group linked to the 6-carbon of the phorbol residue.

Abstract: The present invention relates to novel derivatives of 18?-glycyrrhetinic acid and methods of synthesising the derivatives. Also included within the scope of the present invention are pharmaceutical compositions comprising the derivatives of the present invention and medical uses of the derivatives, including their use in inhibiting enzymes such as retinol dehydrogenases. The present invention also relates to methods of treating diseases, such as hyperproliferative diseases, neoplasms, cancers and photoageing.

Abstract: A process for permeation enhanced reactive extraction of levulinic acid from a liquid aqueous phase comprising levulinic acid, wherein the levulinic acid from the aqueous phase is brought into contact with a liquid alcohol phase at esterification conditions in the presence of a catalyst at a temperature in the range of from 50 to 250° C., the aqueous phase and the alcohol phase being separated from each other by a membrane, and an aqueous stream depleted in levulinic acid and an alcohol stream comprising ester of levulinic acid are formed.

Abstract: The present invention provides a method for the preparation of compounds of formula (II). The invention also provides novel compounds of formula (II) and their use in medical, scientific and/or biological applications.

Abstract: A substituted cyclopentanone represented by the following formula (2): (wherein R3 and R4 represent a substituent having 1 to 8 carbon atoms, may be the same as R1 and R2, respectively, and may be the same as each other) can be produced by hydrogenating the double bond in a compound represented by the following formula (1): (wherein R1 and R2 represent a substituent having 1 to 8 carbon atoms) in the presence of a transition metal catalyst by using a carboxylic acid or a specific concentration of a carboxylic acid ester as a solvent. This process can produce a substituted cyclopentanone which is useful as a jasmine fragrance, an intermediate thereof or the like, in a simple and inexpensive manner at a high cis-isomer ratio.

Abstract: A novel keto8enic compound is provided having general: Formula R(OCH(CH3)CH2C(O))n—O-A wherein n is an integer of 3 to 10, A is the residue of a 3-keto alkan-1-ol and R is selected from the group consisting of H, C1-C6 alkyl and acetoacetyl- Preferred compounds are those wherein A is a residue is of 4-hydroxy-2 butanone. A particularly preferred compound is a 4-hydroxy-2-butanone ester of an R-3-hydroxybutyrate oligomer having general: Formula H(OCH(CH3)CH2C(O))n—O—CH2—CH2—(CO)—CH3 Nutraceutical and pharmaceutical compositions are provided for use in treating one or more of acute trauma, hemorrhagic shock, neurodegeneration, diabetes, and epilepsy, stroke, head trauma, myocardial infraction, congestive heart failure, pulmonary failure, kidney failure, obesity depression, pain and impaired cognition.

Abstract: Carbonyl compounds of the formula (II), wherein R1 and R2 are as defined herein, react in the presence of an amine with carboxylic acid derivatives of the formula (II), wherein R3 and EWG are also as defined herein, to give ?,?-unsaturated compounds of the formula (I) according to the following scheme: It is possible under mild reaction conditions to obtain unsaturated esters with high (E) stereoselectivity. The reaction typically proceeds at room temperature or lower without particular requirements such as inert gas, exclusion of moisture, heat, etc., being made. The only by-products obtained are CO2 and water.

Abstract: Use of a compound of formula 1 as malodour neutraliser wherein A, B, Y and Y have the same meaning as given in the specification, and personal care products comprising the same.

Abstract: The present disclosure provides ketoreductase enzymes having improved properties as compared to a naturally occurring wild-type ketoreductase enzyme. Also provided are polynucleotides encoding the engineered ketoreductase enzymes, host cells capable of expressing the engineered ketoreductase enzymes, method of using the engineered ketoreductase enzymes to synthesize a variety of chirally pure compounds, and the chirally pure compounds prepared therewith.

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract: Isotopically labeled alpha-keto acids and esters are disclosed herein. Also disclosed are methods of synthesizing isotopically labeled alpha-keto acids and esters.

Abstract: A process for the reactive extraction of levulinic acid from an aqueous mixture having levulinic acid, wherein the aqueous mixture is contacted with a liquid esterifying alcohol, the alcohol having at least four carbon atoms and is substantially water-immiscible, at esterification conditions in the presence of a catalyst to form a levulinate ester, wherein the amount of the alcohol is such that the alcohol extracts the levulinate ester from the aqueous mixture. Further, an aqueous phase, having the catalyst and a reduced levulinic acid content, and an organic phase, having the alcohol and the levulinate ester, are formed.

Abstract: A method for the production of 6,6,6-trihalo-3,5-dioxohexanoic acid esters of formula (I): in addition to the enols thereof and <I>E</I> and <I>Z</I> isomers, wherein X independently represents fluorine, chlorine or bromine and R1 represents alkyl, cycloalkyl, aryl or aralkyl. A method for the production of enol ethers of formula (Ib): and the enols thereof (E and Z isomers) wherein X and R1 have the above-mentioned meanings.

Abstract: A process by which an ?-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 ?-oxocarbonyl compound represented by the general formula (I) wherein R1 and R2 are as defined in the description, comprises oxidizing an ?-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).

Abstract: A method for the production of 6,6,6-trihalo-3,5-dioxhexanoic acid esters of formula (I): in addition to the enols thereof and <I>E</I> and <I>Z</I> isomers, wherein X independently represents fluorine, chlorine or bromine and R1 represents alkyl, cycloalkyl, aryl or aralkyl. A method for the production of enol ethers of formula (Ib): and the enols thereof (E and Z isomers) wherein X and R1 have the above-mentioned meanings.

Abstract: A method for obtaining a 5-bromolevulinic acid methyl ester or a 5-chlorolevulinic acid methyl ester from either a bromination mixture or a chlorination mixture, containing either a 5-bromo-levulinic acid methyl ester or a 5-chlorolevulinic acid methyl ester, respectively, produced by either brominating or chlorinating levulinic acid or a levulinic acid methyl ester, and further including the steps of dissolving the bromination or chlorination mixture in an organic solvent or solvent mixture and cooling the solution, preferably to ?20° C.–?40° C., with the 5-bromolevulinic acid methyl ester or 5-chlorolaevulinic acid methyl ester being crystallized out of the solution. The 5-bromolevulinic acid methyl ester or 5-chlorolevulinic acid is then isolated by draining off the solution with the remaining bromination mixture or chlorination mixture, as appropriate.