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Method for producing aqueous acrylamide solution

Tue, 16 Jun 2015 08:00:00 EDT

There is provided a method for producing an aqueous acrylamide solution by reacting a composition including acrylonitrile with water to produce acrylamide, in which the composition including acrylonitrile includes 3 to 15 mg of propionitrile per 1 kg of the total weight of the composition including acrylonitrile. According to the present invention, a production method with which it is possible to suppress acrylamide polymerization without lowering quality and thereby obtain a stable aqueous acrylamide solution can be provided.



Process for making nitriles

Tue, 26 May 2015 08:00:00 EDT

The present invention relates to a process for hydrocyanating 3-pentenenitrile. The process can include feeding 3-pentenenitrile and HCN to a hydrocyanation reaction zone that includes a Lewis acid promoter, nickel, and a phosphorus-containing ligand. In various embodiments, the process can also include controlling water concentration within the hydrocyanation reaction zone sufficient to maintain a high activity of the ligand catalyst complex while recycling at least a portion of the ligand catalyst complex.



Process for making nitriles

Tue, 26 May 2015 08:00:00 EDT

Adiponitrile is made by reacting 3-pentenenitrile with hydrogen cyanide. The 3-pentenenitrile is made by reacting 1,3-butadiene with hydrogen cyanide and by isomerizing 2-methyl-3-butenenitrile. The reaction of 1,3-butadiene with hydrogen cyanide to produce 3-pentenenitrile also produces small amounts of dinitrile compounds, including adiponitrile (ADN) and methylglutaronitrile (MGN). Methylglutaronitrile is removed to provide an adiponitrile-enriched stream, which is used in a catalyst purification step.



Process for making nitriles

Tue, 26 May 2015 08:00:00 EDT

An improved multi-reaction zone process provides for improved nitrile product quality and yield. In a first reaction zone, 1,3-butadiene is reacted with hydrogen cyanide in the presence of a catalyst to produce pentenenitriles comprising 3-pentenenitrile and 2-methyl-3-butenenitrile. In a second reaction zone, 2-methyl-3-butenenitrile, recovered from the first reaction zone, is isomerized to 3-pentenenitrile. In an optional third reaction zone, 3-pentenenitrile recovered from the first and second reaction zones is reacted with hydrogen cyanide in the presence of a catalyst and a Lewis acid to produce adiponitrile. A portion of the first catalyst is purified and recycled. Zero valent nickel is added to the purified first catalyst before it is recycled.



Process for preparing diaryl carbonates from dialkyl carbonates

Tue, 26 May 2015 08:00:00 EDT

The invention provides a process for preparing diaryl carbonates from dialkyl carbonates and aromatic hydroxyl compounds using at least two reaction columns, a process section for recovering the dialkyl carbonate used in the reaction and for removing the alcohol of reaction, one or more process steps for removing the by-products obtained in the process which have a boiling point between that of the dialkyl carbonate and that of the alkyl aryl carbonate formed during the preparation of the diaryl carbonate, and a process step for further purification of the diaryl carbonate obtained from the reaction columns.



Halo active aromatic sulfonamide organic compounds and uses therefor

Tue, 26 May 2015 08:00:00 EDT

Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. This disclosure deals with the use of halo active aromatic sulfonamide organic compounds as odor control and/or biocidal agents in a cleaning solution for use with bovines and other dairy animals.



Method of preparing functionalized graphene

Tue, 26 May 2015 08:00:00 EDT

A method of preparing functionalized graphene, comprises treating graphene with an alkali metal in the presence of an electron transfer agent and coordinating solvent, and adding a functionalizing compound. The method further includes quenching unreacted alkali metal by addition of a protic medium, and isolating the functionalized graphene.



Method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles and use thereof

Tue, 19 May 2015 08:00:00 EDT

The invention relates to a method for producing mono-aminofunctionalized dialkylphosphinic acids and esters and salts thereof by means of acrylnitriles, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) to yield an alkylphosphonic acid, salt or ester (II) thereof in the presence of a catalyst A, b) the thus obtained alkylphosphonic acid, salt or ester (II) thereof is reacted with an acrylnitrile of formula (V) to yield a mono-functionalized dialkylphosphinic acid derivative (VI) in the presence of a catalyst B, and c) the thus obtained mono-functionalized dialkylphosphinic acid derivative (VI) is reacted to yield a mono-aminofunctionalized dialkylphosphinic acid derivative (III) in the presence of a catalyst C or a reduction agent, wherein R1, R2, R3, R4, R5, R6, R7 are the same or different and stand independently of each other, among other things, for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl and X stands for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonized nitrogen base, and Y stands for a mineral acid, a carboxylic acid, a Lewis acid or an organic acid, n=an integer or fractional number of 0 to 4 and the catalysts A and C are formed by transition metals, transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand, and catalyst B is formed by compounds forming peroxides, peroxo compounds, azo compounds, alkali metals, alkaline earth metals, alkali hydrides, alkaline earth hydrides and/or alkali alcoholates and alkaline earth alcoholates.



Preparation method of aromatic boronate compounds

Tue, 19 May 2015 08:00:00 EDT

Preparation method of aromatic boronate compound is provided, in which the is as follows: reacting aromatic amine Ar-NH2, with diboronic ester and alkyl nitrite in the presence of organic solvent, where Ar represents non-heterocyclic aryl. It enables for the first time the preparation of aromatic boronate from aromatic amine in one step by the present method.



Synthesis of H-phosphonate intermediates and their use in preparing the herbicide glyphosate

Tue, 19 May 2015 08:00:00 EDT

The esterfication of hypophosphorous acid is followed by reaction with another molecule of alcohol under the action of a nickel catalyst to provide a green method for the preparation of H-phosphonate diesters. This method avoids the need for any stoichiometric chlorine unlike those based on phosphorous trichloride.



Preparation of nitrile compounds

Tue, 19 May 2015 08:00:00 EDT

The invention relates to novel nitrile compounds according to formula I and II: (I) Formula I wherein: X=—CH3 or —C≡N, (II) Formula II wherein: X=—CH3 or —C≡N, each Y is independently chosen from —OH or RC(0)0-, each R is independently chosen from a C1-21 alkyl group. The invention also relates to processes for the preparation of nitrile compounds according to formula I and II and to uses of the nitrile compounds.



Method for preparing high purity mono-hydrolyzed acyl halide compound

Tue, 12 May 2015 08:00:00 EDT

A method for preparing a high purity (e.g. greater than 70 wt. %) mono-hydrolyzed acyl halide compound as a precipitate from solution comprising the steps of preparing a solution comprising: i) at least 80 v/v % of a hydrocarbon solvent, ii) water at a molar concentration greater than its solubility limit within the solvent but less that its solubility limit in solution, iii) a tri-hydrocarbyl phosphate compound, and iv) a polyfunctional acyl halide compound at molar ratio to both water and the tri-hydrocarbyl phosphate compound of at least 1:1.



***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***Method for producing aqueous acrylamide solution

Tue, 12 May 2015 08:00:00 EDT

There is provided a method for producing an aqueous acrylamide solution by reacting a composition including acrylonitrile with water to produce acrylamide, in which the composition including acrylonitrile includes 3 to 15 mg of propionitrile per 1 kg of the total weight of the composition including acrylonitrile. According to the present invention, a production method with which it is possible to suppress acrylamide polymerization without lowering quality and thereby obtain a stable aqueous acrylamide solution can be provided.



Substituted phenoxyethyl (isopropyl) acyloxyalkyl phosphonate comprising phosphorusheterocyclic ring and having herbicidal activity, and preparation therefor

Tue, 12 May 2015 08:00:00 EDT

A substituted phenoxyethyl(isopropyl)acyloxyalkyl phosphonate having phosphorusheterocyclic ring and having herbicidal activity, with a general formula of I, wherein R represents 5,5-dimethyl-1,3,2-dioxaphosphorinan-2-one-2-yl, or 1-oxo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl, or 1-sulfo-1-phospha-2,6,7-trioxabicyclo 2,6,7-trioxabicyclo[2,2,2]octan-4-yl; R1 represents H, C1-C4 alkyl, phenyl, furyl, pyridyl, or phenyl substituted with methyl, methoxyl, nitro or chloro; R2 represents H, methyl, and methyl only if R in the general formula I is 1-sulfo-1-phospha-2,6,7-trioxabicyclo[2,2,2]octan-4-yl as phosphorusheterocyclic ring; X and Y represent H, halogen, C1-C4 alkyl or trifluoromethyl, and X and Y are the same or different. The compounds according to the present invention may be used as active component of dicotyledonous broadleaf weed herbicides.



Sorafenib derivatives as sEH inhibitors

Tue, 12 May 2015 08:00:00 EDT

The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.



Crystalline form of 3-methylsulfonylpropionitrile

Tue, 05 May 2015 08:00:00 EDT

The present invention relates to processes for preparing 3-methylsulfonylpropionitrile. The processes provide a good yield and a good purity of the final product and provide a controllable reaction. The present invention also relates to a crystalline form of 3-methylsulfonylpropionitrile having X-ray diffraction peaks at 13.9±0.1, 19.2±0.1, 20.0±0.1, 22.5±0.1, 23.2±0.1, 25.7±0.1, 28.1±0.1, 29.9±0.1, and 30.6±0.1 degrees 2θ, and wherein the most intense peak is the peak at 13.9±0.1 degrees 2θ.



Acetaminophen conjugates, compositions and methods of use thereof

Tue, 05 May 2015 08:00:00 EDT

Acetaminophen conjugates are provided, which have an acetaminophen moiety covalently linked to a second moiety. The conjugates provided may have one or more advantageous properties, including increased water solubility as compared to acetaminophen, reduced toxicity profile as compared to acetaminophen and an altered pharmacokinetic profile. Formulations comprising the conjugates are also provided, as are methods of using the conjugates and kits comprising the conjugates.



Process for production of purified O-(2,6-dichloro-4-methyl-phenyl) O,O-dimethyl phosphorothioate

Tue, 05 May 2015 08:00:00 EDT

A process for producing a purified O-(2,6-dichloro-4-methylphenyl)-O,O-dimethyl phosphorothioate, the process comprising: the first step of bringing a crude O-(2,6-dichloro-4-methylphenyl)-O,O-dimethyl phosphorothioate into contact with an acid; andthe second step of recovering the purified O-(2,6-dichloro-4-methylphenyl)-O,O-dimethyl phosphorothioate from the mixture obtained in the first step.



Nickel compositions for preparing nickel metal and nickel complexes

Tue, 05 May 2015 08:00:00 EDT

Nickel(II) compositions for use in manufacturing nickel metal (Ni(0)) compositions, and specifically to methods of making basic nickel carbonates used to produce nickel metal compositions are disclosed. By varying the molar ratios of carbonates and bicarbonates to nickel salts, the methods provide basic nickel carbonates that produce superior nickel metal-containing solids that are well-suited to forming nickel-ligand complexes with phosphorus-containing ligands. The phosphorus-containing ligands can be monodentate or bidentate phosphorus-containing ligands.



Nitrate esters and their use for the treatment of muscle and muscle related diseases

Tue, 05 May 2015 08:00:00 EDT

Alkyl nitrate ester compounds are provided for the delivery of nitric oxide to targeted muscle tissues, and in particular, to normal and dystrophic muscles. In one aspect, nitrate ester compounds are provided having the following formula: wherein, R1 is ONO2, CH2ONO2, CnH2n+1OH, CnH2n+1OH, or CH2CH2CH3, or H;R2 is ONO2, CH2ONO2, Cn′H2n′+1OH, Cn′H2n′+1OH, CH2CH2CH3 or H; andR3 is ONO2, CH2ONO2, Cn′″H2n″+1OH, Cn″H2n″+1OH, CH2CH2CH3 or H; wherein n is an integer from 0 to 9, n′ is an integer from 0 to 9, and n″ is an integer from 0 to 9, and n+n′+n″≦9, and wherein at least one of R1, R2, and R3 is an ester nitrate selected from the group consisting of ONO2, CH2ONO2, and combinations thereof.



Substituted phenylcarbamoyl alkylamino arene compounds and N,N'-BIS-arylurea compounds

Tue, 05 May 2015 08:00:00 EDT

Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N′-substituted aryl urea compounds; N-substituted aryl, N′-substituted heteroaryl urea compounds; N-substituted aryl, N′-substituted aryl thiourea compounds and N-substituted aryl, N′-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.



Radiation-sensitive composition, and compound

Tue, 05 May 2015 08:00:00 EDT

A radiation-sensitive composition includes a compound represented by a formula (1), and a polymer having a structural unit that includes an acid-labile group. In the formula (1), R1 represents a group having a polar group; n is an integer of 1 to 4, wherein, in a case where R1 is present in a plurality of number, the plurality of R1s are identical or different, and optionally at least two R1s taken together represent a cyclic structure; A represents an alicyclic hydrocarbon group having a valency of (n+1); and M+ represents a monovalent onium cation.



Method for the production of alkylphosphonic acids, esters, and salts by oxidizing alkylphosphonous acids, and use thereof

Tue, 28 Apr 2015 08:00:00 EDT

The invention relates to a method for producing monocarboxy-functionalized dialkylphosphinic acids, esters, and salts, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) in the presence of a catalyst A to obtain an alkylphosphonous acid, the salt or ester (II) thereof, and b) the obtained alkylphosphonous acid, the salt or ester (II) thereof is reacted with an oxidizing agent or with an oxidizing agent and water or with oxygen and water in the presence of a catalyst B to obtain the alkylphosphonic acid derivative (III), wherein R1, R2, R3, R4 are identical or different from each other and independently represent, inter alia, H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl, X and Y are identical or different from each other and independently represent H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonated nitrogenous base, and catalysts A and B are transition metals and/or transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand.



Aliphatic polycarbonate quench method

Tue, 21 Apr 2015 08:00:00 EDT

The present disclosure is directed to, in part, an aliphatic polycarbonate polymerization reaction initiated by combining an epoxide with carbon dioxide in the presence of a catalytic transition metal-ligand complex to form a reaction mixture, and further quenching that polymerization reaction by contacting the reaction mixture with an acid containing a non-nucleophilic anion produces a crude polymer solution with improved stability and processability.



Ethyl (2R)-2-acetamido-3-(4-methylbenzoylsulfanyl)propanoate and uses thereof

Tue, 21 Apr 2015 08:00:00 EDT

A novel substituted N-acetyl-L-cysteine (NAC) derivative and methods of using this compound for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.



Organophosphorus compounds, catalytic systems comprising said compounds and method of hydrocyanation or of hydroformylation using said catalytic systems

Tue, 21 Apr 2015 08:00:00 EDT

Organophosphorus compounds, catalytic systems comprising a metallic element forming a complex with the organophosphorus compounds and methods of hydrocyanation and of hydroformylation employed in the presence of the catalytic systems are described.



Fluorescent nanoprobe for detecting hydrogen peroxide and fabrication method thereof

Tue, 21 Apr 2015 08:00:00 EDT

The present disclosure relates to a sulfonated benzene compound emitting fluorescence by reaction with hydrogen peroxide, aqueous-dispersed fluorescent nanoprobes applicable for real-time detection of hydrogen peroxide, and a fluorescent nanoprobe fabrication method. The fluorescent nanoprobe contains the following sulfonated benzene compound and water.



Extraction solvent control for reducing stable emulsions

Tue, 21 Apr 2015 08:00:00 EDT

Disclosed herein are methods for recovering diphosphite-containing compounds from mixtures comprising organic mononitriles and organic dinitriles, using liquid-liquid extraction. Also disclosed are treatments to enhance extractability of the diphosphite-containing compounds.



Process for the production of high-purity dimethyl carbonate

Tue, 14 Apr 2015 08:00:00 EDT

A process for producing a high-purity dimethyl carbonate, which includes: (I) cooling a commercial grade dimethyl carbonate containing 1 ppm or more of chlorine to a temperature from +6° C. to −5° C. at a rate from 0.5-2° C./hour, to obtain a first solid dimethyl carbonate; (II) heating the first solid dimethyl carbonate to a temperature from −5° C. to +6° C. at a rate of 1-5° C./hour, to obtain a mixture comprising a second solid dimethyl carbonate and a predetermined amount of a first liquid dimethyl carbonate; (III) separating the first liquid dimethyl carbonate from the mixture, to obtain the second solid dimethyl carbonate; (IV) heating the second solid dimethyl carbonate to a temperature from 20° C. to 40° C., to obtain a second liquid dimethyl carbonate, wherein the second liquid dimethyl carbonate has a purity degree higher than 99.99% and a chlorine content lower than or equal to 1 ppm.



Oligomer-foscarnet conjugates

Tue, 14 Apr 2015 08:00:00 EDT

The invention relates to (among other things) oligomer-foscarnet conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated foscarnet compounds.



Method for producing silica-supported catalyst, and method for producing unsaturated carboxylic acid or unsaturated nitrile

Tue, 07 Apr 2015 08:00:00 EDT

A method for producing a silica-supported catalyst comprising Mo, V. Nb, and a component X (Sb and/or Te) to be used in a vapor phase catalytic oxidation or ammoxidation of proprane, comprising the steps of: (I) preparing a raw material mixture solution by mixing Mo, V, Nb, component X, a silica sol, and water;(II) obtaining a dry powder by drying the raw material mixture solution; and(III) obtaining a silica-supported catalyst by calcining the dry powder, wherein the silica sol contains 10 to 270 wt ppm of nitrate ions based on SiO2.



Process for preparing triorgano borates with low alcohol content

Tue, 07 Apr 2015 08:00:00 EDT

The present invention provides a process for preparing triorgano borates with low alcohol content.



Process for the preparation of 2-cyanophenylboronic acid and esters thereof

Tue, 07 Apr 2015 08:00:00 EDT

The present invention relates to a process for the synthesis of 2-cyanophenylboronic acid and the esters and salts thereof of formula (II), which are intermediates of the synthesis of active pharmaceutical ingredients such as Perampanel or E2040. formula (II): (II).



Process for the preparation of fluoroalkyl (fluoro)alkyl carbonates and carbamates

Tue, 07 Apr 2015 08:00:00 EDT

Fluoroalkyl alkyl carbonates and fluorosubstituted carbamates which are suitable as additives or solvents in lithium ion batteries are prepared from fluoroalkyl fluoroformates and the respective alcohol or amine. Methanol is the preferred alcohol, dimethylamine and diethylamine are preferred amines. Fluoromethyl methyl carbonate is the preferred compound to be produced. Fluoroalkyl fluoroformates can be prepared from aldehydes and carbonyl fluoride.



Monocyclic cyanoenones and methods of use thereof

Tue, 07 Apr 2015 08:00:00 EDT

The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.



Phosphazene compound having vinyl group, resin composition containing the same, and circuit board manufactured from the same

Tue, 07 Apr 2015 08:00:00 EDT

A phosphazene compound having a vinyl group is manufactured by a reaction between a vinyl compound and a phosphazene compound having a hydroxyl group and added to a resin composition for manufacturing a prepreg or a resin film so as to be applicable to copper-clad laminates and printed circuit boards to thereby achieve satisfactory circuit laminate properties, namely low coefficient of thermal expansion, low dielectric properties, heat resistant, fire resistant, and halogen-free.



Precursors of glutamate derivatives

Tue, 07 Apr 2015 08:00:00 EDT

This invention relates to novel precursors suitable for 18F radiolabeling of glutamate derivatives, methods for preparing such compounds and its intermediates, compositions comprising such compounds, kits comprising such compounds or compositions and methods for 18F radiolabeling of glutamate derivatives wherein the obtained 18F radiolabeled glutamate derivatives are suitable for diagnostic imaging by Positron Emission Tomography (PET) of proliferative diseases e.g. tumor in mammals.



Oxidized thiophospholipid compounds and uses thereof

Tue, 07 Apr 2015 08:00:00 EDT

Novel oxidized thiophospholipids are provided herein, as well as methods for producing same, and uses thereof in treating or preventing an inflammation associated with endogenous oxidized lipids and related conditions. Exemplary oxidized thiophospholipid according to embodiments described herein have the formula: wherein X1, X2, A1, A2, B′, B″, D′ and D″ are as described herein.



Composition that can be cured by polymerisation for the production of biodegradable, biocompatible, cross-linkable polymers on the basis of polyvinyl alcohol

Tue, 07 Apr 2015 08:00:00 EDT

The present invention relates to a polymerization-curable composition for the preparation of biodegradable, biocompatible, cross-linked polymers on the basis of polyvinyl alcohol comprising: 5 to 100% by weight of (a) vinyl ester monomer(s) of one of the general formulas (I) to (III): wherein X is oxygen, sulfur, nitrogen, or phosphorus; n is 1 to 1000, at least 20% of the n being ≧2; the R1 are selected from hydrogen; straight, branched or cyclic, saturated or unsaturated, n-valent hydrocarbon groups having 1 to 30 carbon atoms, which optionally have heteroatoms and are optionally substituted with one or more substituents selected from —OH, —COON, —CN, —CHO, and ═O, and n-valent radicals of biodegradable, biocompatible oligomers and polymers; m is an integer from 1 to 5; the R2 are selected from hydrogen, —OH, ═O, and the options listed for R1; and the R3 are selected from hydrogen, —OH, and the options listed for R1; 0 to 50% by weight of ethylenically unsaturated co-monomers; 0 to 10% by weight of (a) polymerization initiator(s); and 0 to 95% by weight of solvent(s).



Isomerized alpha olefin sulfonate and method of making the same

Tue, 31 Mar 2015 08:00:00 EDT

The present invention is directed to an isomerized alpha olefin sulfonate and a method of making the same wherein the isomerized alpha olefin sulfonate is derived from sulfonating an isomerized alpha olefin with sulfur trioxide in the presence of air thereby producing an isomerized alpha olefin sulfonic acid, wherein the isomerized alpha olefin is derived from the isomerization of C12-C20 normal alpha olefins; and neutralizing the isomerized alpha olefin sulfonic acid with a source of an alkali metal or ammonium or substituted ammonium ion.



Carbonate prodrugs and methods of using the same

Tue, 31 Mar 2015 08:00:00 EDT

The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.



Aminohydroxylation of alkenes

Tue, 24 Mar 2015 08:00:00 EDT

The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.



Point of use generation of amyl nitrite

Tue, 24 Mar 2015 08:00:00 EDT

The present disclosure relates to devices and methods for the preparation of amyl nitrite formulations at a point of use location from relatively shelf-stable reagents employing acidic cationic exchange resins.



Diamino acid derivative starting material, manufacturing method thereof, and diamino acid derivative manufacturing method

Tue, 24 Mar 2015 08:00:00 EDT

Provided is an efficient technology for synthesizing diamino acids (diamino acid derivatives). Disclosed is a manufacturing method for diamino acid derivatives wherein the fluorenyl groups of the diamino acid derivative starting materials represented by General Formula [II] or [IV] are removed.



Isocyanate and isothiocyanate compounds for cancer treatment

Tue, 24 Mar 2015 08:00:00 EDT

The present invention relates to novel isocyanate and isothiocyanate compounds, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans and animals. The novel isocyanate and isothiocyanate compounds are distinguished, as compared with the known isocyanate and isothiocyanate compounds, by improved therapeutical breadth, i.e. fewer side effects while having high anti-tumor activity.



Process of producing phosphinothricin employing nitrilases

Tue, 17 Mar 2015 08:00:00 EDT

The present invention generally relates to processes for the enzymatic production of a phosphinothricin product or precursor thereof from a nitrile-containing substrate.



I-and II-type crystals of L-A-glyceryl phosphoryl choline, and method for preparing same

Tue, 17 Mar 2015 08:00:00 EDT

The present invention relates to I- and II-type crystals of L-α-glyceryl phosphoryl choline, and to a method for preparing same. More particularly, the present invention relates to noble I- and II-type anhydride crystals of L-α-glyceryl phosphoryl choline, which have a higher purity than conventional liquid L-α-glyceryl phosphoryl choline, and one advantage of which is that formulations and dosages of pharmaceuticals are easily modified, and another advantage of which is that the hygroscopicity of the crystals are much lower than that of conventional polymorphic crystals, providing excellent stability during storage. The present invention also relates to a method for preparing the I- and II-type crystals of L-α-glyceryl phosphoryl choline. The I-type crystal of L-α-glyceryl phosphoryl choline is characterized by having an onset temperature of 147° C. and an absorption peak of 150° C. based on differential scanning calorimeter (DSC) analysis, and by having diffraction patterns where 2θ-diffraction angles are 9.8±0.2°, 12.0±0.2°, 14.3±0.2°, 15.8±0.2°, and 19.6±0.2° based on X-ray diffraction (XRD) analysis. The II-type crystal of L-α-glyceryl phosphoryl choline is characterized by having an onset temperature of 62° C. and an absorption peak of 66° C., and an onset temperature of 141° C. and an absorption peak of 145° C. based on DSC analysis, and having diffraction patterns where 2θ-diffraction angles are 10.3±0.2°, 12.2±0.2°, 13.4±0.2°, 14.8±0.2°, and 20.6±0.2° based on XRD analysis.



Catalytic system for CO2/epoxide copolymerization

Tue, 17 Mar 2015 08:00:00 EDT

The present invention related to a method of manufacturing a polycarbonate including the process of copolymerizing epoxide compound and CO2 using cobalt(III) or chromium(III), where the ligands contains at least 3 ammonium cations, central metal has formal −1 charge, and conjugated anions of the two cationic ammonium groups are acid-base homoconjugation, as catalyst. According to the present invention, the initial induction time can be reduced when the said polycarbonate is manufactured and it is possible to improve the activity of the catalyst and the molecular weight of the obtained polymer.



Synthesis of and curing additives for phthalonitriles

Tue, 17 Mar 2015 08:00:00 EDT

A composition having a mixture of the below compounds having a mole ratio of at least 1:20. Ar1 and Ar2 are independently selected aromatic groups. A composition comprising phthalonitrile compounds that comprise at least 5 mol % of the first compound below. A method of: providing a solution of a dichloroaromatic compound having an electron-withdrawing group bound to each aromatic ring containing one of the chloride groups; a dihydroxyaromatic compound or anion thereof; an organic transition metal complex or a transition metal salt; an alkaline hydroxide base; and a solvent; and heating the solution to a temperature at which the dichloroaromatic compound and the dihydroxyaromatic compound react to form a dimetallic salt of an aromatic ether oligomer. The molar ratio of the dihydroxyaromatic compound to the dichloroaromatic compound is greater than 2:1. Water formed during the heating is concurrently distilled from the solution.



Addition-fragmentation agents

Tue, 17 Mar 2015 08:00:00 EDT

Addition-fragmentation agents of the formula are disclosed having the following functional groups: 1) a labile addition-fragmentation group that can cleave and reform to relieve strain, 2) a free-radically polymerizable group, and 3) a surface-modifying functional group that associates with the surface of a substrate.