9 results about "Dihydropyran" patented technology

Provided herein are compounds of Formula (II) (e.g., Formula (II-a), (II-b), (II-a1), (II-b1), (II-a2), (II-b2), (II-3), (II-a3), (II-4), (II-a4), (II-5), (II-a5), (II-6), (II-a6), (II-7), (II-a7), (II-7), or (II-a8)), Formula (III) (e.g., Formula (III-1), (III-2), (III-3), (III-4), (III-5), (III-6), (III-7), or (III-8)), Formula (IV) (e.g., Formula (IV-a), (IV-b), (IV-c), (IV-a1), (IV-b1), (IV-a2), (IV-b2), (IV-a3), (IV-b3), (IV-a4), (IV-b4), (IV-a5), (IV-b5), (IV-a6), (IV-b6), (IV-a7), (IV-b7), (IV-a8), or (IV-b8)), Formula (V) (e.g., Formula (V-a) or (V-b), (V-a1), (V-c), (V-d), (V-b1), (V-a2), (V-b2), (V-a3), or (V-b3)), Formula (VI) (e.g., Formula (VI-a), (VI-b), (VI-c), (VI-d), or (VI-e))), or Formula (A) (e.g., Formula (I-a1)), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein (e.g., a dysregulated KRas protein (e.g., a mutated or amplified KRas protein)). This disclosure also provides compositions containing the compounds as provided herein, or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

This disclosure relates to a hair care composition comprising a compound that can covalently bond to hair and an excipient suitable for administration to hair, wherein the compound that can covalently bond to hair is a compound of formula (I), or its tautomers and / or pharmaceutically acceptable salts, where (I), R 1 L1 represents a protecting group that can be hydrolyzed under physiological conditions after application of hydrogen or a hair care composition to the hair, L1, L2 and L3 independently represent a linker group or are absent, and A1, A2 and A3 independently represent a)C1~C 30 Partial, H, hydroxyl, amino, or halogen, or b) C1-C 60 Represents a part or polymer part, and at least one of A1, A2 and A3 is C1-C of group b). 60 It is a part or polymer part, and C1-C of group b) 60 The present invention relates to a hair care composition in which the polymer portion is configured to act as b1) a humectant, a hair beautifying coating, or a primer for adhering dye to hair, and / or b2) a humectant, a hair beautifying coating, or a fragrance for cleavage from the 3,4-dihydro-2H-pyran portion, and L1-A1 and L2-A2 do not represent portions containing an unsaturated CC bond or CN bond at the alpha position to the carbon atoms marked "a" and "b", respectively. [Formula 1] JPEG2026520679000070.jpg29128

The application discloses a preparation method of a medical intermediate (R)-7-ethyl camptothecin, and relates to the field of chemical medicine synthesis. The application comprises the following contents: (R)-4-ethyl-4-hydroxy-7,8-dihydro-1H-pyrano[3,4-f]indolizine-3,6,10(4H)-trione (formula A) and 1-(2-aminophenyl)propan-1-one (formula B) are used as main raw materials, a target compound (R)-7-ethyl camptothecin is obtained through reaction in an organic solvent under the action of a catalyst. The application provides a novel preparation method of the medical intermediate (R)-7-ethyl camptothecin, and the preparation method is simple, stable, high in yield, and suitable for industrial production.

The application relates to a method for synthesizing dihydropyrrolo[2,3-c]pyrazole analogs. Specifically, under the catalysis of a transition metal and a bidentate ligand, dihydropyrrolo[2,3-c]pyrazole analogs can be obtained in high selectivity by using the bidentate ligand synergy, taking pyrazolinone as raw material and reacting with 1,3-alkyne under the action of triethylenediamine. The application uses cheap and commercially available 1,3-alkyne and easily obtained pyrazolinone, and a series of heterocyclic compounds with potential medicinal value are obtained in high selectivity under simple and mild conditions.

This invention provides a ketone reductase mutant and its application in the synthesis of a key chiral intermediate for ticoraxene. The mutant contains amino acid sequences such as SEQ ID NO: 4, 6, 8, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, or 42. This ketone reductase mutant exhibits higher carbonyl catalytic activity and chiral selectivity than the wild type, and is used in the preparation of the key intermediate R-5,7-difluorobenzodihydropyran-4-ol for ticoraxene.

The present invention is entitled "A Continuous Flow Preparation Method for Tegoragen Intermediates", belonging to the field of chemical synthesis technology. The technical problem to be solved is that the existing preparation methods have safety risks, long reaction time and low yield. The key points of the technical solution are as follows: The continuous flow preparation method of the present invention is as follows: (1) 3,5-difluorophenol and 3-chloropropanol are dissolved in organic solvents to form solutions, and then reacted with organic amines in a microreactor. After the reaction is completed, the material is discharged and the organic layer 1 is separated; (2) 2,2,6,6-tetramethylpiperidine oxide is added to the organic layer 1, and then reacted with sodium hypochlorite solution and sodium chlorite solution in a microreactor for oxidation reaction. After the reaction is completed, the material is discharged and the organic layer 2 is separated; (3) The organic layer 2 is then reacted with concentrated sulfuric acid in a microreactor. After the reaction is completed, the material is washed with water and the organic layer 3 is separated. After concentration and recrystallization, the tegoragen intermediate 5,7-difluorobenzodihydropyran-4-one is obtained.

The application belongs to the technical field of green organic chemistry, and particularly relates to a method for catalytically preparing 2-amino-3-cyano-4,8-dihydropyrano[3,2-b]pyran. The method uses aromatic aldehyde, malononitrile and kojic acid as reaction raw materials, uses taurine bisulfate as a catalyst, uses water as a reaction solvent, and reacts at a certain temperature. After the reaction is completed, the reaction system is cooled to room temperature, filtration is performed, the solid crude product is separated, and then the corresponding 2-amino-3-cyano-4,8-dihydropyrano[3,2-b]pyran compound pure product can be obtained through ethanol recrystallization and vacuum drying. The application has the advantages of good biocompatibility of the catalyst, good catalytic activity, recyclability and the like, and the whole preparation process is simple, convenient, easy to realize large-scale industrial application.

Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds are (3-aryl-1,2,4-oxadiazol-5-yl)-3,4-dihydro-2H-pyrano[2,3-b]pyridines of the following structure:in which Ar is aryl or heteroaryl. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2 / Smad3 signaling pathway.