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).

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

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 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.

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.

In a process for the separation and drying of crude carboxylic acid crystals from a slurry in a solvent, the slurry is supplied to a filter operating at pressure and at a temperature above the atmospheric boiling point of the solvent. A cake of separated crystals is removed from the filter and passed to a thermal dryer. In a system for the separation and drying of crude carboxylic acid from a slurry in a solvent, a pressure filter device has a slurry inlet and an outlet for a cake of carboxylic acid crystals. The system also has a thermal dryer and means for transporting the cake of carboxylic acid crystals from the pressure filter device to the dryer. The pressure filter device is configured to operate at a pressure and temperature above the atmospheric boiling point of the solvent.

A thermal separation process between a gas ascending in a separating column and a liquid descending in the separating column, which comprise (meth)acrylic monomers, wherein the separating column comprises a sequence of crossflow mass transfer trays, the crossflow mass transfer trays of which have passage orifices for the ascending gas in crossflow direction both in front of and beyond a downcomer for the descending liquid, and such crossflow mass transfer trays and one such crossflow mass transfer tray in a sequence of crossflow mass transfer trays present in a separating column.

A process for preparing a pure alanylglutamine comprises the steps of: 1) reacting N-(α-chloro)-propionyl-glutamine and hydrazine compound to obtain an alanylglutamine crude product; 2) mixing anhydrous methanol and the alanylglutamine crude product to provide a filter cake; 3) dissolving the filter cake in water, heating, adding ethanol, and cooling to yield the pure alanylglutamine.

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.

In a process for removing aromatic carboxylic acid from a slurry thereof in solvent, the slurry is split into sub streams and each of said sub streams is supplied to a respective rotary pressure filter such that the sub stream pass through the filters in parallel. Gas is passed through the rotary pressure filters in series in an open-loop arrangement.

A method of preparing the anthracyclin carminomycin using a starting material comprising daunorubicin. The method comprises reacting daunorubicin or N-protected daunorubicin with soft Lewis acids for the demethylation of the 4-methoxy group, resulting in a reaction mass. The reaction mass is treated with an aqueous solution of a strong organic acid or a mineral acid. After decomposition of the resulting carminomycin and Lewis acids reactive complex, the reaction mass is extracted using a water insoluble organic solvent. As a result, carminomycin is extracted as a base.

Disclosed is a method of preparing cationic starch. The method includes preparing a starch suspension containing a cationization agent; performing ultrahigh pressure treatment on the starch suspension; and obtaining cationic starch from the starch suspension subjected to ultrahigh pressure treatment.

A cytosine analog, a method of preparation of a cytosine analog, a DNA methyltransferase 1 inhibitor, and a method for DNA methylation inhibition, is provided for the treatment of diseases associated with deviations from normal DNA methylation. The analog of cytosine may be comprised of 1, N4, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formula where R1 is H, R3, R4, 2'-deoxyribosyl, R4 is alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then R5 is no substituent and if X in the analog of formula I and/or II is C or if X in the analog of formula II is N, then R5 and R6 are independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.

Non-ionic water-soluble cellulose ethers modified with 3-azido-2-hydroxypropyl groups bound via an ether link are provided having a molar degree of substitution MSAHP in the range from 0.001 to 0.50. Exemplary cellulose ethers are alkyl celluloses, including methyl, hydroxyalkyl (e.g. hydroxyethyl or hydroxypropyl) or alkylhydroxyalkyl cellulose (e.g. methylhydroxyethyl). Reaction products with alkyne compounds are also provided, resulting in a terminal alkyne group. The reaction of azide with the alkyne proceeds as a 1,3-dipolar cycloaddition reaction, advantageously with Cu(I) or ruthenium catalysts. A multiplicity of cellulose ethers can be obtained from the conversion reaction. Variations in the macroscopic properties can be achieved by controlled modification, ranging from increased or reduced viscosity. The reaction, taking place within a few seconds, requires only minimal catalyst. Gel formation is reversible by adjustment of the pH such that a monophasic system (high-viscous fluid) arises again from a biphasic system (gel+low-viscous water phase).

The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.

A method for continuously preparing a carboxylic acid ester is disclosed. In the method of the present invention, a vertical reactor is filled with a solid catalyst, a carboxylic acid and an alcohol are introduced into a lower part of the vertical reactor, esterification is performed to form an esterized mixture, the esterized mixture is output from an upper part of the vertical reactor, and distillation is performed to isolate the carboxylic acid ester. The method of the present invention is simple, easily controlled and environmental friendly, and has significantly high conversion rate and selectivity.

A process for preparing an ester of formula (I): R3CH2—(CR1R2)n—CH2—O—CO—(CR1R2)n—CH2R3 (I) wherein n is 1-3 and R1 and R2 are each, independently, a hydrogen atom or a carbon-linked organic group and R3 is a carbon-linked organic group, is provided by hydrogenation of a certain lactone, carboxylic acid or its ester reactant.

The present invention provides drug conjugates comprising 5-aminolevulinic acid (ALA), an aldehyde and a carboxylic acid that may function as a histone deacetylase inhibitor (HDACI). These conjugates may serve as co-drugs which release a plurality of active species in vivo. The novel drug conjugates may be used, for the treatment or prevention of cancer in PDT-dependent and/or PDT-independent (nonPDT) treatments, as well as for cosmetic uses. In addition the present invention provides novel uses for both the novel and known compounds. According to some embodiments, the present invention provides drug conjugates (co-drugs) comprising (i) ALA, (ii) an aldehyde and (iii) a carboxylic acid that may function as a histone deacetylase inhibitor (HDACO for the treatment of anemia and/or for the induction of erythropoiesis.

The invention relates to a process for preparing pentabromobenzyl acrylate through the reaction of pentahalobenzyl halide with a salt of acrylic acid in water-immiscible solvent, wherein said salt is in aqueous form and the reaction is carried out in the presence of a phase transfer catalyst. A process for polymerizing the pentabromobenzyl acrylate in halogenated aromatic solvent and the poly (pentabromobenzyl acrylate) obtained are also disclosed.

Aromatic isocyanates are produced by reacting one or more aromatic primary amines with phosgene in the gas phase. The phosgene and primary aromatic amine(s) are reacted at a temperature above the boiling temperature of the amine(s) in a reactor having a reaction space which is essentially rotationally symmetric to the direction of flow. The flow fate, averaged over the cross-section, of the reaction mixture along the axis of the essentially rotationally symmetric reaction space in the section of the reaction space in which the conversion of the amine groups into isocyanate groups is between 4 and 80% is not more than 8 m/sec. The flow rate averaged over the cross-section of the reaction mixture along the axis of the essentially rotationally symmetric reaction space in the section of the reaction space in which the conversion of the amine groups into isocyanate groups is 4 to 80% is always below the flow rate averaged over the cross-section at the start of this section.

Provided is a gem-dinitro ester compound, represented by Formula 1 below: wherein R is a substituted or unsubstituted straight-chain or side-chain alkyl group of C2˜C12.

The present invention relates to a process of making a compound of formula (I): Wherein, R1, R2, R4 and X are as defined herein.

Isocyanates are produced in the gas phase and by-products such as ammonium halides are selectively separated from the gas phase by desublimation.

The present invention relates to a covalently organo-modified LDH (LDH/APTES) was found to be an efficient and reusable heterogeneous catalyst for C—C bond forming reactions (i.e. Aldol condensation, Knoevenagel condensation, Henry reaction, Michael addition). More particularly, this catalyst shows consistent activity for several cycles in C—C bond forming reaction. These catalysts were successfully characterized by XRD, FT-IR, 29Si CP MAS NMR.

The present invention relates to norbornene-ester-based derivatives, to a method for preparing same, and to the uses thereof. This compound may be used as a plasticizer which can replace a phthalate-based plasticizer.

Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.

This disclosure relates to a method for preparing alkyl lactate with high yield and high selectivity, comprising the step of reacting glycerol with water or alcohol in the presence of a catalyst. In addition, the present invention provides a method for efficiently preparing lactamide using the alkyl lactate.

A process to prepared bridged bis(indenyl)ligands, comprising the step of reacting a 2-indenylpinacolyl borane compound with a bromosubstituted compound in the presence of a Pd catalyst and a base to form the corresponding bridged bis(indenyl) ligand. The process may further comprise the step of reacting a 2-bromo indene compound with pinacolborane in the presence of a Pd catalyst and a base to form the corresponding 2-indenylpinacolylborane compound. These bridged bis(indenyl)ligands may suitably be used in the preparation of metallocene complexes, such as 2,2'-bis(2-indenyl)biphenyl ZrCl2 and 1,2-bis(2-indenyl)benzene ZrCl2. These metallocene complexes may be used for the polymerization, optionally in the presence of a cocatalyst, of one or more α-olefins, preferably for the polymerization of ethylene.

A method of continuously manufacturing organometallic compounds is provided where two or more reactants are conveyed to a reactor having a laminar flow contacting zone, a heat transfer zone, and a mixing zone having a turbulence-promoting device; and causing the reactants to form the organometallic compound.

An efficient process for synthesizing phosphaplatins in large quantities is disclosed by adding platinum complex to a concentrated pyrophosphate solution at pH from between about 6.0 to 8.5. After stirring, the temperature and pH are lowered to precipitate out desired phosphaplatins. Particularly, the disclosed processes reduce the need to use large volumes of starting materials, and shorten the reaction time. In addition, disclosed is a process for recycling un-reacted materials from a first phosphaplatins synthesis.

A method of making amino-mercapto functional organopolysiloxanes is disclosed by reacting (A) a dialkoxydialkylsilane, (B) an amino functional alkoxy silane, and (C) a mercapto functional alkoxy silane, via a condensation reaction. The amino-mercapto functional organopolysiloxanes products are useful in textile and fabric treatments.

A combination of a substrate selected from silicon, silicon carbide or a metal and a grapheme precursor having the following properties: (a) an aromatic structure that forms the basis of the graphene structure, said aromatic structure being selected from the group consisting of: benzene, naphthalene, pyrene, anthracene, chrysene, coronene, and phenanthrene, or a cyclic or acyclic structures which can be converted to aromatic structures and (b) functional groups that can react with each other to form additional aromatic structures.

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.

A method for forming a cobalt-containing thin film by a vapor deposition process is provided. The method comprises using at least one precursor corresponding in structure to Formula (I); wherein R1 and R2 are independently C2-C8-alkyl; x is zero, 1 or 2; and y is zero or 1; wherein both x and y can not be zero simultaneously.

A method of preparing organohalosilanes comprising combining an organohalide having the formula RX (I), wherein R is a hydrocarbyl group having 1 to 10 carbon atoms and X is fluoro, chloro, bromo, or iodo, with a contact mass comprising at least 2% (w/w) of a palladium suicide of the formula PdxSiy (II), wherein x is an integer from 1 to 5 and y is 1 to 8, or a platinum suicide of formula PtzSi (III), wherein z is 1 or 2, in a reactor at a temperature from 250 to 700° C. to form an organohalosilane.

The present invention relates to a novel compound of Formula 1, a method for manufacturing the same, and an organic electronic device using the same, and the novel compound according to the present invention may act as a hole injection, hole transport, electron injection and transport, or light emitting material in an organic light emitting device and an organic electronic device, and the device according to the present invention shows excellent properties in terms of efficiency, a driving voltage, and stability.

Method for preparing diamino-dianhydro-dideoxyhexitols, particularly 2,5-diamino-1,4:3,6-dianhydro-2,5-dideoxy-D-hexitol. The invention related to a method for preparing diamino-dianhydro-dideoxyhexitols, particularly preferably 2,5-diamino-1,4:3,6-dianhydro-2,5-dideoxy-D-hexitol.

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.

A process for the preparation of 1,3:2,4-bis(4-methylbenzylidene)sorbitol (MDBS) and 1,3:2,4-bis(3,4-dimethylbenzylidene)sorbitol (DMDBS) via a dehydrocondensation reaction is disclosed. The reaction is carried out between an aldehyde and an alditol in a mole ratio of 2:1 wherein ionic fluid is used as the acidic catalyst and/or reaction medium. The ionic fluid used in accordance with the present invention is quaternary ammonium salt based ionic liquid.

A method is provided for the preparation of anhydrosugar alcohols. The method involves dehydration of a hexitol with a mixed acid of a first acid and second acid, in which the first acid is sulfuric acid and the second acid is at least one sulfur-containing acid or sulfur-containing acid salt selected from the group consisting of p-toluenesulfonic acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, naphthalenesulfonic acid and aluminum sulfate. Also provided are methods for purification of the resulting product.

The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.

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.

Provided are a method of preparing a chlorohydrin composition and a method of preparing epichlorohydrin by using a chlorohydrin composition prepared by using the method. The method of preparing chlorohydrins in which polyhydroxy aliphatic hydrocarbon is reacted with a chlorination agent in the presence of a catalyst includes performing at least one combination of a series of unit operations comprising a first reaction step, a water removal step, and a second reaction step in this stated order, wherein the method further includes mixing a chlorohydrin concentrate obtained by purifying the reaction mixture discharged from the final reaction step from among the reaction steps and a water-rich layer discharged from the water-removal step and diluting the mixture with water. The method of preparing epichlorohydrin includes contacting the chlorohydrin composition prepared by using the method of preparing a chlorohydrin composition with an alkaline agent.

The present invention relates to the preparation of cyclopropane derivatives, in particular 2-amino-9-[[(1S,2R)-1,2-bis(hydroxymethyl)cyclopropyl]methyl]-4,8-dihydro-1H-purin-6-one, especially via the [(1S,7R)-4-phenyl-3,5-dioxabicyclo[5.1.0]octan-1-yl]methanol intermediate.

An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

The present invention relates to a process for the preparation of 17α-(3-hydroxypropyl)-17β-hydroxysteroids of the formula I starting from 17-ketosteroids of the formula III via the intermediates of the formula V wherein the radicals R3, R5, R6, R7, R10, R13, R15, R16, R40, R41 and R42 have the meaning indicated in the description.

The present invention relates to processes for the crystallisation and for the preparation and isolation of a novel crystalline form of fusidic acid, to the use of said processes in the manufacture of pharmaceutical formulation or medicament, and to the use of said crystalline fusidic acid form for the treatment of bacterial infections.

The present invention discloses novel process for the preparation of (2R)-2-acetamido-N- benzyl-3-methoxypropanamide of Formula I involving novel intermediates of Formula-XIX and Formula-XX.

Suspension concentrate compositions are disclosed for delivering S-(+)-Abscisic acid either alone or in combination with a second plant growth regulator to crop seed prior to planting as well as for foliar, soil drench, in-furrow and sprench (foliar spray and soil drench) applications are disclosed. The compositions, when properly combined in an aqueous carrier and processed through wet milling to achieve the desired particle size, will result in stable compositions that are desirable for treating crop seeds.