13 results about "Isoindoles" patented technology

The invention belongs to the technical field of medicine synthesis processes, and particularly relates to a preparation method of high-yield and high-purity tandospirone citrate. According to the method, pyrimido piperazine quaternary ammonium salt and isoindoledione are used as raw materials, a toluene and n-butanol and / or n-amyl alcohol mixed solvent is used as a solvent, tandospirone can be generated under the alkaline condition without adding a phase transfer catalyst, after acid adjustment extraction and specific organic solvent reverse phase impurity removal, a water phase is adjusted to be alkaline, and the tandospirone is obtained. And extracting with toluene, and adding a citric acid ethanol solution to directly separate out a citric acid tandospirone solid. The preparation process disclosed by the invention has a very good impurity removal effect, and the obtained tandospirone citrate is high in purity, high in process yield, good in atom economy and low in output of three wastes.

The invention relates to a compound of formula (I) wherein n = 1 or 2, A and A'are independently selected from the group consisting of the following substituents (II-a) and (II-b), R and R 'are independently selected from H and a linear or branched C1-C3 alkyl group, Z is selected from a linear or branched C1-C4 alkyl group and an aryl group optionally substituted by a linear or branched C1-C3 alkyl group and / or by a hydroxyl group, and the structural unit of formula (N) is selected from the following structural units (III-a), (III-b), (III-c), (III-d) and (III-e) wherein for each structural unit (III-a), (III-b), (III-c), (III-d) and (III-e), Ra, Rb, Rc and Rd are independently selected from a linear or branched C1-C4 alkyl group. .

The invention discloses a benzoxazino isoindolone compound as well as a synthesis method and application thereof, and belongs to the field of organic synthesis. A 2-aryl benzoxazine compound 1 and a fluoro methyl acetylenic ketone compound 2 are used as raw materials, and in the presence of a rhodium catalyst, an additive and an organic solvent, a temperature rise reaction is performed to obtain the benzoxazino isoindolone compound 3. A plurality of groups of compounds are screened, and antiviral and anticancer activity tests verify that the compound provided by the invention has the activity of obviously inhibiting proliferation of three cancer cells such as the Zika virus and Hela, A549 and HCT-116, so that the compound provided by the invention has the activity of resisting the Zika virus and has the anticancer activity on cervical cancer, lung cancer and colon cancer.

2-(Piperidin-3-yl)isoindole-1,3-dione analogs and uses thereof are disclosed. The compounds have a structure according to Formula I, or a stereoisomer or pharmaceutically acceptable salt, solvate, or hydrate thereof. The compounds may be useful for inhibiting TNF-α activity, TNF-α synthesis, interleukin-6 (IL-6) level, inflammation, or SARS-COV-2 virus. In some aspects, the compounds, or pharmaceutical compositions including the compounds, are administered to a subject a traumatic brain injury (TBI), an inflammatory disorder, a neurodegenerative disease, cancer, a viral infection, or any combination thereof.

The present invention relates to a method for treating a tumor such as a tumor with a KRAS mutation. In the method, a compound 2-fluoro-5-methoxy-4-[(4-(2-methyl-3-oxo-2,3-dihydro-1H-isoindole-4-oxy)-5-trifluoromethyl-pyrimidine-2-yl)amino]-N-(1-methyl-piperidine-4-yl)benzamide or a pharmaceutically acceptable salt thereof is used, which can be administered alone or in combination with a KRAS inhibitor and / or an MEK inhibitor.

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2 (1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

The application discloses a preparation method of lenalidomide, which comprises the following steps: S1, methyl 2-bromomethyl-3-nitrobenzoate, 3-aminopiperidine-2,6-dione hydrochloride and a base are dissolved in a polar solvent, and reaction is carried out at 50-60 DEG C for 5-8 h; after the reaction is completed, the obtained mixed product is refined and purified to obtain 3-(7-nitro-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione; S2, 3-(7-nitro-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione, ammonium formate and a palladium-carbon catalyst are added into a mixed solvent, and reaction is carried out at 35-45 DEG C for 4-7 h; after the reaction is completed, the obtained crude product is further treated; S3, the crude product is stirred and dissolved in a polar solvent, and then filtered; ammonium formate and sodium mercaptoacetate are added into the filtrate, and reaction is carried out under stirring for 2-5 h; after the reaction is completed, the obtained mixed solution is refined and purified to obtain lenalidomide.

A method for electrochemically driving 2-(1-alkynyl)benzamide derivative to cyclize and synthesize iodoisoindolone, in which 2-(1-alkynyl)benzamide derivative and tetrabutylammonium iodide are used in an electrolyte and a solvent at room temperature to obtain iodoisoindolone. The electrochemical driving efficiency is higher, the substrate conversion rate is increased to 95%, heavy metal residues are avoided, the requirements of drug intermediates are met, no temperature control energy consumption is needed, the process is simplified, the efficiency is improved, and the functional group tolerance is better.

The application discloses application of a benzimidazole amine derivative in preparation of an antitumor pharmaceutical composition, in particular, application of a benz(4,5)imidazo(2,1-a)isoindole-2-methylprop-2-amine derivative in preparation of an antitumor pharmaceutical composition. The benz(4,5)imidazo(2,1-a)isoindole-2-methylprop-2-amine derivative provided by the application has a significant inhibiting effect on colon cancer, liver cancer, lung cancer, prostate cancer, cervical cancer, neuroglioma and breast cancer, shows excellent antitumor characteristics, can be used as a leading drug molecule for resisting tumors, and has a good development and application prospect in development of antitumor drugs.

The invention belongs to the field of organic synthesis, and particularly relates to a synthesis method of isoindolone. N-methylbenzylamine derivative as shown in formula 1, N-methyl-N-(4-pyridylmethyl) amine as shown in formula 4, N-methyl-2-thiophenemethylamine as shown in formula 6, 2-methoxy methyl benzoate derivative as shown in formula 2 and 2-methoxy methyl nicotinate pyridine as shown in formula 9 in bis (trimethylsilyl) The method comprises the following steps of: mixing and reacting with an organic solvent methyl tert-butyl ether in the presence of a catalyst, lithium amide and a cesium fluoride additive to synthesize isoindolone as shown in a formula 3, isoindolone as shown in a formula 5, isoindolone as shown in a formula 7 and isoindolone as shown in a formula 10.

The invention provides an application of 4-bromo-N-(1-methyl-3-(4-methylbenzoyl)-2H-isoindole-2-yl) benzenesulfonamide in preparation of an antitumor drug, and relates to the technical field of biomedicine. The invention provides an excellent potential of 4-bromo-N-(1-methyl-3-(4-methylbenzoyl)-2H-isoindoline-2-yl) benzenesulfonamide (ISO-1 for short) in the aspect of resisting colon cancer, and a cell experiment carried out by a CCK-8 method in the application shows that the ISO-1 has a direct killing effect on colon cancer MC38 cells. In a mouse colon cancer model constructed by MC38 cells, the treatment effect of the ISO-1 is further confirmed. Experimental results show that compared with an untreated Control group, the tumor volume of each group of mice treated by ISO-1 is obviously reduced. The ISO-1 treatment obviously prolongs the lifetime of tumor-bearing mice. The lifetime is one of gold standards for measuring the effectiveness of anti-cancer drugs.

The application discloses a tin-titanium oxide catalyst and a preparation and application thereof. The catalyst is obtained by calcining after mixing titanium oxide and an organic tin compound uniformly, the catalyst takes the titanium oxide as a carrier and loads the tin dioxide, and the loading mass of the tin dioxide accounts for 20-30% of the mass of the catalyst. Furfurylamine and acrylic acid are reacted in a solvent and the catalyst in a reaction kettle at a certain temperature for a certain time to obtain isoindole ketone. The method has the advantages of high isoindole ketone yield, simple and easily obtained raw materials, simple operation, economy, environmental protection and wide substrate applicability.