es

Defoamer compositions for building-product mixtures

The present application relates to compositions comprising at least one siloxane and at least one superplasticizer based on polycarboxylate ethers or sulphonates of lignin, melamine or naphthalene or of resins thereof, and to the use of such compositions as or in building-product mixtures or building products, especially mortar mixtures or concrete mixtures. Preferably the siloxane is a branched siloxane containing at least one “T” unit and containing at least two different polyoxyalkylene moieties.




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Method of synthesising polycarbonates in the presence of a bimetallic catalyst and a chain transfer agent

The invention provides a process for the synthesis of a polycarbonate, the process comprising the step of reacting carbon dioxide with at least one epoxide in the presence of a catalyst of formula (I) and a chain transfer agent. The invention also provides a polymerization system for the copolymerization of carbon dioxide and at least one epoxide comprising a catalyst of formula (I) and a chain transfer agent, polycarbonates produced by the inventive process, a block copolymer comprising a polycarbonate produced by the inventive process, and a method of producing the block copolymer. The invention also relates to novel catalysts of formula (III).




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Electroluminescent display useful for displaying a predetermined pattern

An electroluminescent display comprising semiconductor nanocrystals, wherein the semiconductor nanocrystals are selected to emit light at a predetermined wavelength and are disposed in a predetermined pattern. In certain embodiments, semiconductor nanocrystals that emit light at different predetermined wavelengths are disposed in the display to create a predetermined multi-color pattern.




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Efficient processes for large scale preparation of phosphaplatins antitumor agents

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.




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Process for preparing amino-mercapto functional organopolysiloxanes

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.




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Synthesis and applications of peripherally asymmetric aryl POSS compounds

Asymmetric aryl polyhedral oligomeric silsesquioxanes (ArPoss) compounds synthesized by the “corner-capping” of phenyl7Si7O9(OH)3 with aryl trichlorosilanes are described. The ArPoss compounds have the chemical structure: wherein Ph is phenyl and wherein R is selected from the group consisting of: and mixtures thereof.




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Transition metal complexes for inhibiting resistance in the treatment of cancer and metastasis

The present invention relates to organometallic compounds useful in the treatment of metastasis. The organometallic compounds comprise a ligand that is covalently bound to a bioactive compound, which is an inhibitor of a resistance pathway or a derivative thereof. Preferably, the organometallic compounds are half-sandwich (“piano-stool”) compounds. The compounds of the present invention offer a high variability with respect to the bioactive compound and to the nature of the ligand bound to a central transition metal.




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Functionalized polyhedral octavinylsilsesquioxanes and a method to obtain the functionalized polyhedral octavinylsilsesquioxanes

A new functionalized polyhedral octavinylsilsesquioxanes having the general formula 1, in which R1 denotes: (1) any aryl group other than a non-substituted phenyl or a phenyl substituted in position four with a halogen or the groups-trimethylsilylethynyl, 4,4,5,5-tetramethyl-1,3-dioxaborolane-2-yl, 3,4-dimethoxyphenyl, 3',5'-bis(methoxycarbonyl)phenyl or benzo[d][1,3]-dioxol-5-yl; (2) any heteroaryl group; or (3) groups including coupled aromatic rings. Additionally, a method to obtain new and known functionalized polyhedral octavinylsilsesquioxanes having the general formula 1, by the silylating coupling of octavinylsilsesquioxane with olefins in the presence of a ruthenium complex catalyst.




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Stereoselective synthesis of bridged metallocene complexes

The present invention provides methods of making stereo-enriched ansa-metallocene compounds using an unchelated amine compound. Generally, these methods result in a rac:meso isomer selectivity of the stereo-enriched ansa-metallocene compound of greater than 4:1.




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

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.




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Nickel compositions for preparing nickel metal and nickel complexes

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.




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Hydrophobic, functionalized particles

The present invention relates to a stable mixture comprising surface-modified particles which are obtained by reacting metal oxide or semimetal oxide particles with at least one compound selected from among silicon-comprising compounds bearing at least one metaloxy radical and optionally further alkoxy and/or hydroxy radical(s) and at least one solvent, at least one surface-active substance or a mixture thereof, a process for producing the mixture, the use of these particles in systems in which they are brought into contact with at least one solvent, where the mass ratio of solvent to modified particle is greater than 500, and also the use of these particles in agglomeration-deagglomeration cycles.




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High molecular weight alkyl-allyl cobalttricarbonyl complexes and use thereof for preparing dielectric thin films

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.




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Mixtures of silicon-containing coupling reagents

Mixtures of silicon-containing coupling reagents comprising (mercaptoorganyl)alkylpolyethersilanes containing silanol groups and (mercaptoorganyl)alkylpolyethersilanes free of silanol groups in a weight ratio of from 5:95 to 95:5. The mixtures can be prepared by transesterification and hydrolysis. The mixtures can be used in rubber mixtures.




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Ruthenium catalysts and their use for asymmetric reduction of ketones

Disclosed are novel ruthenium compounds of formula (Ia) and (Ib): wherein R1 and the moiety are defined herein. Also disclosed is a process for using these novel ruthenium compounds as catalysts for asymmetric hydrogenation and transfer hydrogenation of ketones with high reactivities and excellent selectivities.




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Process for production of cyclic silane compound and/or cyclic carbosilane compound

A process for producing a cyclic silane compound, in which a chained polysilane is subjected to pyrolysis in the presence of an oxide of a transition metal belonging to Group 8 or Group 11 of the periodic table; and a process for producing a cyclic carbosilane compound, that includes subjecting a chained polysilane to pyrolysis in the presence of a simple substance of a metal selected from the group consisting of transition metal elements and elements belonging to Groups 12 to 15 of the periodic table, or a compound thereof.




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Silanes with embedded hydrophilicity, dispersible particles derived therefrom and related methods

The invention provides a silane compound that includes a hydrophobic group and a silane ester group linked by a hydrophilic group for use as a surface treatment to an inorganic material, such as a pigment, the silane including a hydrophobic group and a silane ester group linked by a hydrophilic group. The invention includes a coated particle including an inorganic material coated with the silane compound(s) and methods of improving the wettability and/or dispersibility of an inorganic material such as a pigment, wherein the method comprises depositing the silane compounds on the surface of a pigment.




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Organosilicon compounds and their use for producing hydrophilic surfaces

Compounds of the formula where R1 each individually is identical or different and is a hydrocarbon radical, R2 each individually is hydrogen or a methyl radical, n is an integer from 6 to 11, and m is 0 or 1, with the proviso that the sum of the number of carbon atoms in the three radicals R1 in the compound of the formula (I) is 6 to 24, can be admixed with curable polymer compositions to form products with hydrophilic surfaces, or can be applied to surfaces to render them hydrophilic.




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Process for recovering homogeneous metal hydride catalysts

The present invention relates to a process for recovery of homogeneous metal hydride catalyst from a reactor stream as catalyst suitable for recycle to a reactor comprising the steps of: removing a stream from a reactor, said stream comprising the homogeneous metal hydride catalyst; contacting the stream with a solid acidic absorbent under process conditions which allow at least some of the metal to become bound to the absorbent; subjecting the metal bound to the absorbent, under process conditions which allow desorption of the metal, to a fluid stripping medium comprising hydrogen and solvent; and recovering the active metal hydride catalyst.




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Synthesis of phosphinimide coordination compounds

Methods to make R13P═N—TiCl3 and (1-R2-Indenyl)Ti(N═PR13)Cl2, where R1 is independently selected from C1-30 hydrocarbyl radical which is unsubstituted or further substituted by one or more halogen atom, a C1-8 alkoxy radical, a C6-10 aryl radical, a C6-10 aryloxy radical, an amido radical, a silyl radical, and a germanyl radical; P is phosphorus; N is nitrogen (and bonds to the metal M); R2 is a substituted or unsubstituted alkyl group, a substituted or an unsubstituted aryl group, or a substituted or unsubstituted benzyl group, wherein substituents for the alkyl, aryl or benzyl group are selected from alkyl, aryl, alkoxy, aryloxy, alkylaryl, arylalkyl and halide substituents. The method to make R13P═N—TiCl3 combines a titanium species TiCl3(OR) where R is an alkyl or aromatic group, with a trimethylsilyl phosphinimide compound R13P═N—SiMe3 in the presence of solvent, to give the titanium complex R13P═N—TiCl3. The method to make (1-R2-Indenyl)Ti(N═PR13)Cl2 consists of deprotonating 1-R2-indene with an appropriate base, followed by reaction with R13P═N—TiCl3.




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

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.




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Apparatus and methods to preserve catalyst activity in an epoxidation process

Apparatus and methods are provided for forming and processing multiphasic systems. In one embodiment, the invention provides a process for the manufacture of an epoxide, including reacting an olefinically unsaturated compound with an oxidant in the presence of a buffer component and a water-soluble manganese complex disposed in an aqueous phase having a first pH level in a first multiphasic system, adjusting the pH of the aqueous phase to a second pH level less than the first pH level, isolating at least a portion of the aqueous phase from the first multiphasic system, adjusting the pH of the at least a portion of the aqueous phase to a third pH level greater than the second pH level, and introducing the at least a portion of the aqueous phase into a second multiphasic system.




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Antioxidant nanosphere comprising [1,2]-dithiolane moieties

The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.




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Silica nanoparticle agent conjugates

The invention provide a silica nanoparticle comprising a non-porous matrix of silicon-oxygen bonds, wherein the matrix comprises organic agents conjugated to silicon or oxygen atoms in the matrix, the organic agents are conjugated to the matrix through linker L groups, wherein the linker L comprises, for example, an ester, urea, thiourea, or thio ether group, and wherein the diameter of the nanoparticle is about 15 nm to about 200 nm. The invention also provides novel methods of making and using the silica nanoparticles described herein.




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Thiophenes and uses thereof

This invention provides thiophene compounds of formula I: wherein R1, R2, R3, R4, n, p, and m are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.




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Rosin derived epoxides and curing agents

An epoxide agent for an epoxy resin system, the epoxide agent comprising at least one non-acid functional rosin moiety and at least one epoxide moiety. Another embodiment is a curing agent for an epoxy resin system comprising at least one non-acid functional rosin moiety and at least one moiety that is reactive with an epoxy.




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***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***Halichondrin B analogs

The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate.




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Bicyclic compound and use thereof for medical purposes

Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.




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Process for preparation of acetals

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.




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5-sec-butyl-2-(2-4-dimethyl-cyclohex-3-enyl)-5-methyl-[1,3]dioxane and process for making the same

The present invention is directed to 5-sec-butyl-2-(2,4-dimethyl-cyclohex-3-enyl)-5-methyl-[1,3]dioxane and a novel process for making the same.




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Method for producing methylene-1,3-dioxolanes

The present invention relates to a novel method for preparing methylene-1,3-dioxolanes of the general formula (I) in which R1 and R2 have the meanings stated in the description. Methylene-1,3-dioxolanes are important intermediates for preparing pyrazoles and anthranilic acid amides, which may be used as insecticides.




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Method of synthesizing low color furan diesters

The present invention relates to a method of making low colored bis(2-ethylhexyl) furan-2,5-dicarboxylate (BEHFD) plasticizer via mild hydrogenation of highly colored BEHFD.




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Oxidation process to produce a purified carboxylic acid product via solvent displacement and post oxidation

Disclosed is a process to produce a dry purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). The process comprises oxidizing at least one oxidizable compound selected from the following group: 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH2-furfural were R alkyl, cycloalkyl and aryl), 5-HMF ethers (5-R'OCH2-furfural, where R'=alkyl, cycloalkyl and aryl), 5-alkyl furfurals (5-R″-furfural, where R″=alkyl, cycloalkyl and aryl), mixed feed-stocks of 5-HMF and 5-HMF esters and mixed feed-stocks of 5-HMF and 5-HMF ethers and mixed feed-stocks of 5-HMF and 5-alkyl furfurals to generate a crude carboxylic acid slurry comprising FDCA.




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Esterification of furan-2,5-dicarboxylic acid to a dialkyl-furan-2,5-dicarboxylate vapor with rectification

A process for the manufacture of dialkyl furan-2,5-dicarboxylate (DAFD) vapor composition by feeding furan-2,5-dicarboxylic acid (“FDCA”) to an esterification reactor and in the presence of an alcohol compound such as methanol, conducting an esterification reaction to form an esterification vapor containing DAFD, unreacted alcohol compound, 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC), and water, and continuously passing the esterification vapor through an ACFC condensing zone, that can be integral with the esterification reactor, in which at least a portion of the ACFC in the esterification vapor is converted to a liquid phase condensate, and continuously discharging the esterification vapor from the ACFC condensing zone as a DAFD vapor. There is also a DAFD vapor composition containing DAFD, water, unreacted alcohol, and by-products.




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Pharmaceutical composition comprising rotigotine salts (acid or Na), especially for iontophoresis

The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol(rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.




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Diphenylmethane derivatives as SGLT2 inhibitors

A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.




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Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors

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.




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Recovery of lactic acid values from a meso-lactide stream

Lactic acid equivalents are recovered from a starting lactide stream by catalytically racemizing a portion of the lactide in the stream at a temperature of 180° C. or below. This increases the proportion of two species of lactide (i.e., at least two of S,S-, R,R- or meso-lactide) at the expense of the third species. The racemized mixture so obtained can be separated to recover some or all of one or more of the lactide species from the remaining lactide species, by a process such as melt crystallization or distillation. Impurities in the starting lactide stream usually are retained mostly in the remaining meso-lactide, so a highly purified S,S- and/or R,R-lactide stream can be produced in this manner. Such a purified S,S- and R,R-lactide stream is suitable for polymerization to form a polylactide.




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Total synthesis of artemisinin

The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as a starting material.




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Crystalline molecular comlpexes of tadalafil

Crystalline molecular complexes of tadalafil are disclosed. The crystalline molecular complexes include those of tadalafil and oxalic acid, tadalafil and 4-hydroxybenzoic acid, tadalafil and 3-phenylpropanoic acid, tadalafil and malonic acid, tadalafil and methylparaben, and tadalafil and propylparaben. Pharmaceutical compositions containing the crystalline molecular complexes are also disclosed.




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Method for preparing cyclopropane derivatives

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.




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Benzocycloheptane and benzoxepine derivatives

The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.




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Process for the preparation of quaternary N-alkyl morphinan alkaloid salts

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




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Histone deacetylase inhibitor of benzamides and use thereof

Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumors, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.




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Process for producing 1,4-butanediol by hydrogenating dialkyl maleate in mixed liquid/vapor phase

A process for the production of 1,4-butanediol and tetrahydrofuran by catalytic hydrogenation of dialkyl maleates includes the following steps: a) hydrogenating a stream of dialkyl maleate in a first stage of reaction over suitable catalysts to produce dialkyl succinate;b) further hydrogenating the dialkyl succinate in a second stage of reaction, by using a different suitable catalyst, for producing mainly 1,4-butanediol, together with gamma-butyrolactone and tetrahydrofuran as co-products. In both stages of reaction the conditions, as hydrogen/organic feed ratio, pressure and temperature, are such to maintain the reactors in mixed liquid/vapor phase.




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Process for the preparation of compounds useful as inhibitors of SGLT

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.




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Steroids having increased water solubility and resistance against metabolism, and methods for their production

Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.




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Process for the preparation of 17-(3-hydroxypropyl)-17-hydroxysteroids

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.




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Synthesis of 7-acetyleno quinone methide derivatives and their application as vinylic polymerization retarders

The invention provides a method for synthesizing 7-Acetyleno quinone methide compounds that is safe and inexpensive. The method avoids the need for extremely cold reaction temperatures and unlike the prior art does not require any highly explosive materials. The method comprises the steps of: a) performing a condensation reaction between 3,5-di-tert-butyl-4-hydroxybenzaldehyde and a secondary amine thereby forming a secondary amine quinone methide intermediate;b) removing water from the secondary amine quinone methide intermediate by azeotropic distillation;c) adding the dehydrated secondary amine quinone methide intermediate to an organic medium containing a metal acetylide to form a Mannich base intermediate; andd) adding a release agent to the Mannich base intermediate to yield a 7-Acetyleno quinone methide.




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C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.