834results about "Sulfonic acid esters preparation" patented technology

The invention provides substituted diaryl compounds as shown in general formula (I) or their pharmaceutically acceptable salts, and also provides a preparation method; a class of novel broad-spectrum antiviral compounds and pharmaceutical salts targeting cytokines are screened and obtained through studies on structure-activity relationship and action mechanism of active compounds; the compounds not only have significant broad-spectrum antiviral activity, but also have the advantages of low toxicity and good pharmaceutical properties.

The radiolabeled non-natural amino acid 1-amino-3-cyclobutane-1-carboxylic acid (ACBC) and its analogs are candidate tumor imaging agents useful for positron emission tomography and single photon emission computed tomography due to their selective affinity for tumor cells. The present invention provides methods for stereo-selective synthesis of syn-ACBC analogs. The disclosed synthetic strategy is reliable and efficient and can be used to synthesize a gram quantity of various syn-isomers of the ACBC analogs, particularly, syn-[18F]-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC) and syn-[123I]-1-amino-3-iodocyclobutane-1-carboxylic (IACBC) acid analogs.

Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and / or toxic compounds and are readily amenable to scale-up.

This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X2 is a halo group, and is —F, —Cl, —Br, or —I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic estenfication (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).

The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of organofluoro compound [18F]florbetaben or [18F]AV-45 having <Chemistry Formula 11> and <Chemistry Formula 12>, respectively, by reacting fluorine salt containing radioactive isotope fluorine-18 with alkyl halide or alkyl sulfonate in the presence of alcohol of Chemistry Formula 1 as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.

A method for the preparation of graphene is provided, which includes: (a) oxidizing a graphite material to form graphite oxide; (b) dispersing graphite oxide into water to form an aqueous suspension of graphite oxide; (c) adding a dispersing agent to the aqueous suspension of graphite oxide; and (d) adding an acidic reducing agent to the aqueous suspension of graphite oxide, wherein graphite oxide is reduced to graphene by the acidic reducing agent, and graphene is further bonded with the dispersing agent to form a graphene dispersion containing a surface-modified graphene. The present invention provides a method for the preparation of graphene using an acidic reducing agent. The obtained graphene can be homogeneously dispersed in water, an acidic solution, a basic solution, or an organic solution.

This invention relates to pharmaceutically acceptable amphiphilic antioxidant compounds, compositions and dosage forms comprising said compounds, and methods and uses reliant on said compounds. The exemplified compounds are all mitoquinone derivatives, being methoxyphenyl alkyl triphenylphosphonium or methoxy dioxocyclohexadiene alkyl triphenylphosphonium derivatives. The compounds, compositions, dosage forms, uses and methods are useful in, for example, the treatment of diseases or conditions associated with oxidative stress.

The invention discloses a novel compound capable of being applied to fluorescent recognition of cysteine and homocysteine, particularly relates to a preparation method and an application of a novel fluorescence probe, and belongs to the technical field of chemical analysis detection. The molecular structural formula of the novel fluorescence probe is as shown in the description. The fluorescence probe can be applied to fluorescent sensing analysis of cysteine and homocysteine in an environment or a biological sample, and has good selectivity on the cysteine and the homocysteine, high anti-jamming capability, and a good application prospect; and the cysteine and the homocysteine can be sensitively and rapidly distinguished out from a plurality of amino acids.

A method for the treatment of carcinoma in a human is disclosed, including administering to a human a therapeutically effective amount of 9-cis, 11-trans octadecadienoic acid formed by reacting an ester of ricinoleic acid with a tosyl chloride or a mesyl chloride to form a tosylate or mesylate of an ester of ricinoleic acid, and reacting the tosylate or mesylate of an ester of ricinoleic acid with diazabicyclo-undecene. The method includes administering to a human a purified conjugated linoleic acid (CLA) produced by a novel synthesis process for producing 9-cis, 11-trans octadecadienoic acid at room temperature in high yield including providing a tosylate or mesylate of a methyl ester of ricinoleic acid and providing a purified 9-cis, 11-trans octadecadienoic acid formed when the tosylate or mesylate reacts with diazabicyclo-undecene.

The invention discloses a method for synthesizing a novel tetracyclic diterpene compound from stevioside, which is cost-efficient and feasible. The compound is represented by a general formula (I), wherein the definitions of R1, R2, X, Y are shown in the specification. The invention discloses a potential application value of the compound in the aspects of anti-tumor and anti-inflammation and a detailed preparation method of the compound as well as physical data of Fourier transform infrared spectroscopy (FT-IR), hydrogen nuclear magnetic resonance spectroscopy (1 HNMR), mass spectrometry (MS) and the like.

The invention relates to the field of chemical synthesis of medicines and in particular relates to a preparation method and intermediate of an AHU-377 intermediate and a preparation method of the intermediate. The preparation method of the AHU-377 intermediate shown in a formula (I) in the description comprises the following steps: performing a substitution reaction on a compound shown in a formula (II) in the description and a compound shown in a formula (III) in the description and then carrying out hydrolysis to prepare the AHU-377 intermediate shown in the formula (I), wherein the hydrolysis reaction is carried out in the presence of hydrogen peroxide and lithium hydroxide hydrate. The invention also aims to provide a new compound with a structure shown in the formula (II). In the new route, as a new compound shown in a formula (IV) in the description is prepared through reaction of the compound in the formula (II) and the compound in the formula (III), the selectivity is quite good, and a few diastereoisomers are generated in the reaction process and can be removed only through simple aftertreatment.

The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu / delta opioid modulators.

The invention relates to side substitution aromatic ester diphenol, a preparation method and a preparation method of a mesomorphic epoxy monomer. The side substitution aromatic ester diphenol has a general formula shown in the specification of the invention, wherein X stands for an aryl group with side substitution. In the preparation method of an aromatic ester mesomorphic epoxy monomer by using the side substitution aromatic ester diphenol, a synthetic period of the monomer is greatly shortened, the raw materials of the synthetic monomer are cheap and are easy to obtain, and the preparation method is simple and convenient.

The present invention relates to a process for efficiently producing an optically active 2-bromocarboylic acid and an optically active 2-sulfonyloxycarboxylic acid, which are important in the production of medicinal compounds and so forth. An optically active 2-sulfonyloxycarboxylic acid ester is subjected to deprotection under acid conditions to obtain an optically active 2-sulfonyloxycarboxylic acid. A metal bromide is caused to act on the acid to brominate it with configuration inversion at position 2 to thereby produce an optically active 2-bromocarboxylic acid. The resultant optically active 2-bromocarboxylic acid is isolated / purified by subjecting it to a step in which the acid is crystallized and separated as a salt with a base. Thus, an optically active 2-bromocarboxylic acid having a high chemical purity and high optical purity can be produced.

An amorphous carbon having sulfonate group introduced therein is provided which is characterized in that chemical shifts of a condensed aromatic carbon 6-membered ring and a condensed aromatic carbon 6-membered ring having sulfonate group bonded thereto are detected in a 13C nuclear magnetic resonance spectrum and that at least a diffraction peak of carbon (002) face whose half-value width (2θ) is in the range of 5 to 30° is detected in powder X-ray diffractometry, and which exhibits proton conductivity. This sulfonated amorphous carbon is very useful as a proton conductor material or solid acid catalyst because it excels in proton conductivity, acid catalytic activity, thermal stability and chemical stability and can be produced at low cost.

A method is disclosed for the production of taurine in high yield by a cyclic process of reacting monoethanolamine, sulfuric acid, and ammonium sulfite in the presence of additives to inhibit the hydrolysis of 2-aminoethyl hydrogen sulfate intermediate. The cyclic process is economical and little waste is generated.

The invention discloses a 3-cyclohexyl-1,1-dimethylurea compound as well as a preparation method and application thereof. The 3-cyclohexyl-1,1-dimethylurea compound is used for preparing an antischizophrenic drug cariprazine. Compared with the prior art and report literatures, the preparation method of the 3-cyclohexyl-1,1-dimethylurea compound has the remarkable advantages of being free of removal of protecting groups such as Boc group, high in atom economy, low in cost and easy in getting of raw materials, mild in reaction condition, stable in yield, simple and convenient to operate, controllable in product quality, high in product purity, less in three waste pollution and easy to produce industrially. The structure formula of the 3-cyclohexyl-1,1-dimethylurea compound is as shown in (I) in the specification.

The invention relates to an asymmetric hydrogenation method of alpha-oxo-alpha, beta-unsaturated carboxylic acid. A metal complex containing ChenPhos chiral ligand is a catalyst high in conversion efficiency, and particularly, the catalyst can be used for synthesizing a core framework in enkephalinase inhibitor Sacubitril through asymmetric hydrogenation. The inhibitor is one of components of medicine LCZ 696 approved by American Food and Drug Administration. The asymmetric hydrogenation method of the alpha-oxo-alpha, beta-unsaturated carboxylic acid is efficient, and the application range of substrate is wide.

The invention discloses a gemini perfluoroalkylsulfonyloxybenzyl cationic surfactant as well as preparation and application thereof. The structural general formula of the surfactant is as shown in a formula I, wherein Rf is perfluorobutylsulfonyl or perfluorohexylsulfonyl; n is 2, 3, 4 or 6; X is a counter anion. The perfluorobutylsulfonyl or the perfluorohexylsulfonyl is a fluorine-containing precursor material; the gemini perfluoroalkylsulfonyloxybenzyl cationic surfactant is obtained through the sulfonation of the fluorine-containing precursor material with p-hydroxybenzylalcohol, chlorination with a halogenating reagent and quaternization with tetramethyl alkyl diamine. The gemini cationic surfactant provided by the invention is free of a perfluorooctyl group with a lasting organic pollutant characteristic, high in surface activity and low in critical micelle concentration; an aqueous film-forming foam fire extinguishing agent obtained by compounding the gemini cationic surfactant with additives is quick in aqueous film-forming spreading speed and excellent in fire extinguishing performance.

The invention discloses a Bilastine preparation method. The Bilastine preparation method includes that 2-nitroaniline which is low in price and easy to obtain is taken as a raw material which is subjected to reduction-n-cyclohexylmaleimide reaction, alkylation reaction, hydrolyzing and coupling prior to hydrolyzing to obtain Bilastine. With the method, shortcomings that harsh operation conditions, high toxicity, expensive raw materials and tedious operation in the prior art are overcome, reaction conditions in each step are moderate, and the synthetic method is simple in operation, easy to deal with, few in side products, high in yield and purity, low in production cost and suitable for industrial production.

Poly-perfluoroalkyl substituted polyethyleneimine compositions are provided that act as foam stabilizers and film formers when used in fire-fighting foam concentrates. The polyethylene compositions are soluble in water, but have only low solubility in polar solvents. When aqueous film forming foam generated from these concentrates is applied to burning polar solvent the polyethyleneimine compositions precipitate at the polar solvent / foam interface and inhibit the collapse and destruction of the foam.

The invention relates to a compound for preparation of cariprazine and a preparation method thereof. The method can overcome the defects in the prior art, the used raw materials and reagents are low toxic, cheap and easily available, the reaction conditions are mild, fewer three wastes are generated, at the same time, the operation is simple and safe, and the yield is good, therefore the method is suitable for industrialized production.

This invention relates to pharmaceutically acceptable amphiphilic antioxidant compounds, compositions and dosage forms comprising said compounds, and methods and uses reliant on said compounds. The exemplified compounds are all mitoquinone derivatives, being methoxyphenyl alkyl triphenylphosphonium or methoxy dioxocyclohexadiene alkyl triphenylphosphonium derivatives. The compounds, compositions, dosage forms, uses and methods are useful in, for example, the treatment of diseases or conditions associated with oxidative stress.

A process of producing N-acyl amino acid based surfactants of Formula I,wherein, R is selected from C6 to C22 alkyl group, R1 is selected from H, C1 to C4 alkyl, R2 is selected from all groups on α carbon of natural amino acids, R3 is selected from COOX, CH2—SO3X, X is selected from Li+, Na+ or K+. The process comprising steps of:A) preparing fatty acid chlorides by halogenating fatty acids with either phosgene or thionyl chloride in the presence of catalytic amount of same or other N-acyl amino acid surfactant of Formula I or anhydrides of same surfactant; andB) reacting fatty acid chloride of step (A) with an amino acid in the presence of a base.

The invention discloses a novel ester group-containing aromatic propionamide compound as well as a preparation method and an application thereof, and provides a chemical structure formula of the novel ester group-containing aromatic propionamide compound. The compound is prepared by taking an acyl chloride compound and proline as starting raw materials. The compound has the effect of adjusting an androgen receptor and can be independently used or being used as a composition to be used for treating and / or preventing various diseases related to androgens, such as diseases of male androgen deficiency (ADAM), diseases of female androgen deficiency (ADIF), muscle consumption, muscle emaciation, amyotrophy, osteoporosis, sclerotin reduction, anemia, obesity, diabetes mellitus, cancers and the like; the compound can also be used for an exercise and / or body function enhancing agent or an animal feed additive.

The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon. The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.