71 results about "Medicinal chemistry" patented technology

A process is provided for preparing spiro-hydantoin compounds of the formula II

wherein Z is N or CR_4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A₂ is a linker, G′ is a linker; Q is a linker; and R₂, R_4a, R_4c, and R_h are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S, 9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.

The invention relates to cariprazine tartrate (I), a crystal form, a preparation method therefor and use of cariprazine tartrate for treating schizophrenia and dual-phase type I disorder drugs. The compound provided by the invention is excellent in water solubility, flowability of powder and stability, and is an excellent medicinal form of cariprazine. The formula is shown in the description.

The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.

The present invention provides a dispersant for aqueous and non-aqueous systems which can disperse insoluble fine powders in aqueous and non-aqueous liquids in a short period of time and give long-term dispersion stability to the resulting dispersions. The dispersant is a compound of the formula

wherein CY is selected from the group consisting of aliphatic monocyclic compounds having one double bond and aliphatic polycyclic compounds with or without one double bond, or with or without bridge carbons; (n+x+y+z)>1; and R=—H, —SO₃M, —CO₂M, —PO₃M, —OCR′ wherein M=H, or Na, K, Li, Ca, Mg, NH4, NH(R₁)₂, NH₂R₁, N(R₁)₃ where R₁ is selected from the group consisting of C₁-C₆ alkyl and C₁-C₆ hydroxyalkyl; and R′=C₂-C₂₂ alkyl or alkenyl.

Disclosed are compounds having the structure:

wherein Z is —OH or —O•; and

A is:

wherein

• • • X and Y are independently NR₁ or O, where
    • R₁ is H or C₁-C₄ alkyl; and
    • R₂ is H, C₁-C₄ alkyl or t-butoxycarbonyl,
    • wherein W is C₃-C₄ alkynyl; and
    • R₁ is H or C₁-C₄ alkyl, or
    • wherein R₁ is H, C₁-C₄ alkyl, or C₃-C₄ alkynyl; and
      • R₃ is H, OH, O(C₁-C₄ alkyl), or a halogen,

optically active enantiomers, pharmaceutically acceptable salts of the compounds, pharmaceutical compositions containing such compounds or salts, and processes for their preparation. The subject invention also provides methods of alleviating symptoms of neurologic, autoimmune, and inflammatory disorders caused by the presence of reactive oxygen species, methods of preventing oxidation of lipids, proteins, or deoxyribonucleic acids on a cellular level, and methods of protecting human red blood cells from lysis by O₂ radicals.

A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I):

wherein X represents a single bond or a C₁ to C₆ alkylene group which may be substituted; A represents a C₁ to C₆ alkyl group which may be substituted, a C₆ to C₁₀ aryl group which may be substituted, or a 4 to 10-membered monocyclic or bicyclic and unsaturated, partly saturated, or completely saturated heterocyclic group which may be substituted, wherein said heterocyclic group comprises as ring-constituting atoms 1 to 4 hetero atoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

The invention discloses a synthetic method for a chiral quaternary carbon oxazolidinone compound. The synthetic method comprises the following steps: taking o-hydroxy chalcone and azlactone as reactants and synthesizing in a solvent under the catalysis of chiral multifunctional chiral quinine thiourea to obtain a product. The synthetic method disclosed by the invention has the advantages that raw materials are easy to obtain, the reaction conditions are mild, the post-treatment is simple and convenient, the applicable substrate scope is wide, the yield is high, and the enantioselectivity is high; the product obtained by the synthesis method can be used for synthesizing an intermediate of a drug and a pesticide.

The invention discloses a method for preparing anhydrous neodymium chloride under an open system, which relates to a method for preparing anhydrous neodymium chloride and aims to solve the problems of vacuum environment requirement and complex preparation process of the traditional method for preparing the anhydrous neodymium chloride. The method for preparing the anhydrous neodymium chloride under the open system, disclosed by the invention, is finished through the following steps of: firstly, preparing neodymium chloride hexahydrate by using neodymium oxide; and secondly, preparing neodymium chloride by using the neodymium chloride hexahydrate: horizontally spreading NH4Cl on a reaction boat; then, horizontally spreading the neodymium chloride hexahydrate on the NH4Cl, then roasting, reacting and then grinding to obtain the anhydrous neodymium chloride. The method is applied to the field of chemical industry.

The invention relates to a novel preparation method of a useful decisive compound of Aluminum Magnesium hydroxy Carbonate serving as a therapeutic agent of gastrointestinal diseases as shown in chemical formula 1.

The invention relates to a preparation method of diphenyl ether dianhydride and isomers thereof, which is characterized in that the preparation method comprises the following steps of: adding solvent and monochlorophthalic anhydride into a reactor with a drying and distilling device, increasing temperature for reflux for a certain period under the protection of N2, adding alkali metal salt and catalysts, conducting reflux reaction for a certain period, decreasing the temperature, conducting filtration to obtain crude products, adding cyanophenyl and the crude products prepared through the reaction into the clean reactor with the drying and distilling device, increasing the temperature for reflux for a certain period under the protection of N2, decreasing the temperature, conducting filtration and drying to obtain the diphenyl ether dianhydride and the isomers thereof. The preparation method provided by the invention has the advantages that the synthesis method of the diphenyl ether dianhydride is widened, the preparation process of the diphenyl ether dianhydride is simplified, the environmental pollution is reduced and a new method is provided for the industrial production of the diphenyl ether dianhydride.

A cured product of a compound of the following formula has a low Abbe number and a high abnormal dispersibility. X and Y are O, S, N or S; Z and X—C═C—Y form 5 to 7-membered ring; R¹ and R² represents H, alkoxy, mercapto, thioalkoxy, amino, alkylamino, carboxy, alkylcarbonyloxy, carbamoyloxy or alkoxycarbonyloxy; and R³ to R⁶ represent substituent.

The invention relates to the technical field of synthetic methods of milnacipran hydrochloride. The preparation method provided by the invention comprises the following steps: carrying out reactions in five steps on an existing compound to generate a novel compound V; and then, reducing the compound V and salifying to obtain the milnacipran hydrochloride. The reactions are simple to operate and mild in condition. The intermediate and final products obtained are high in yield and purity. The invention provides the economic and efficient preparation method of milnacipran hydrochloride, and the method is suitable for industrialized production.

The invention relates to a preparation method of a high activity Pd/C catalyst, and the preparation method is mainly used for solving the problems of poor Pd dispersion in the catalyst, low microcrystal content and poor thermal stability of the prior art. The preparation method adopts activated carbon as a carrier and impregnates or sprays solution containing Pd on the activated carbon for preparing the Pd/C, wherein, two additives of A and B are added in the solution containing Pd, the additive A is selected from compounds with the above formula, R1 or R2 is selected from one of H, CH3, NH2, OH or COOH, n or m is selected from integrals of 0 to 5; the additive B is selected from compounds with the following formula: CH3(CH2)xO(CH2CH2O)yPO(OM)2(CH3(CH2)xO(CH2CH2O)y)2PO(OM), wherein, y is selected from the integrals of 1 to 5; x is selected from the integrals of 7 to 15; M is selected from Na or K; therefore, the technical proposal can better solve the problems and can be used in the industrial production of para-toluic acid catalyst by using 4-carboxy benzaldehyde.

The invention discloses a new process for preparing capecitabine from fluterolone, which belongs to the technical field of medicinal chemistry. It is characterized in that 5'-deoxy-5-fluoro-uridine is used as the starting material, after 2', 3' hydroxyl protection, generation of 5-fluorocytidine, acylation of n-pentyl chloroformate and slight acid removal Capecitabine was obtained by four-step chemical reaction of hydroxyl protecting group. The preparation method has reasonable sequence, stable and easy-to-obtain raw materials, mild reaction conditions, strong process controllability, high yield, high purity intermediate crude product, no cumbersome purification treatment, and is suitable for industrial production.

The present invention relates to a method for preparing diphenylethanone from benzyl alcohol through a photocatalytic one-step method. According to the method, diphenylethanone is directly prepared byusing inexpensive benzyl alcohol as a raw material under the action of a solid photocatalyst; and the reaction process comprises: mixing benzyl alcohol, a catalyst and an acetonitrile solvent are mixed, placing in a pressure container, replacing with an inert gas, and carrying out illumination stirring at a room temperature, wherein the reaction time is more than 1 h, the catalyst is easily separated from the reaction system after the reaction and can be recycled multiple times, and the separation yield of diphenylethanone is up to 81%.