31 results about "Cyclopentamine" patented technology

The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compoundsare useful for the useful for the treatment or prevention of conditions mediated by tachykinins and / or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

The invention discloses a preparation method of a pyridine pyrimidine derivative. The preparation method comprises following steps: 3-methyl-2-glutaconate diester and cyclopentamine are subjected to amidation condensation to prepare 1-cyclopentyl-4-methylpyridine-2, 6-(1H, 5H)-dione, and one-pot condensation with methylation reagent (N, N-dimethylformamide acetal) and urea is carried out so as toobtain 2-hydroxyl-5-methyl-8-cyclopentyl pyridine [2, 3-d] pyrimidine-8-hydro-7-one; and then chlorination and bromination reaction are carried out to prepare 2-chlor-5-methyl-6-bromo-8-cyclopentyl pyridine [2, 3-d] pyrimidine-8-hydro-7-one. The preparation method possesses following advantages: using of expensive trihalogen pyrimidine, palladium salt catalyst, and 3-borate substituted ethyl crotonate is avoided; the adopted raw materials are cheap and easily available; operation is convenient; reaction yield is stable; less three wastes are generated; reaction atom economical benefit is high;cost is low; and the preparation method is convenient for green industrialized production.

The invention discloses methods for preparing 3-cyclopentamine and slats thereof. The method for preparing the 3-cyclopentamine comprises the following steps of: adding cis-1,4-dichloro-2-butene and nitromethane serving as initial raw materials into a solvent to perform a reaction in the presence of an alkaline catalyst and at the temperature of 25 to 80 DEG C to obtain 4-nitro-cyclopentyl-1-alkenyl; and reducing the 4-nitro-cyclopentyl-1-alkenyl in a reduction system to obtain the 3-cyclopentamine. The new process provided by the invention reduces the course for synthesizing the target product to a relatively large extent, successfully solves the problems of high-price, rareness and the like of the raw materials of the target product and avoids a diazotization reaction at the same time. The new process greatly reduces production cost, improves yield and product purity and is simple in operation and convenient for mass production.

The invention relates to the field of drug synthesis, in particular to a preparation method of a palbociclib intermediate. In the preparation method of the present invention, compound I: 2,4-dichloropyrimidine is used as the starting material, replaced by cyclopentylamine, and transesterified with methyl acetoacetate, and then catalyzed by boron trifluoride ether The target compound IV is obtained by ring closure: 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-D]pyrimidinyl-7-one. The synthetic route designed by the invention avoids the use of palladium catalyst, the overall reaction conditions are mild, the reaction yield is high, the production cost is low, it is suitable for industrial production and is environmentally friendly.

The present invention relates to the technical field of medicines, and provides a process for the industrialized preparation of palbocoxib intermediate 5-bromo-2-chloro-4-cyclopentylaminopyrimidine (M1), which comprises the following steps: (1) Under room temperature conditions, select a weakly basic inorganic salt as an acid-binding agent, and use a low-boiling point solvent as a reaction solvent, add cyclopentylamine dropwise to 2,4-dichloro-5-bromopyrimidine (M0), and react for 12-15 hours; (2) Suction filtration to remove inorganic salts, concentrate the mother liquor to dryness, and recrystallize the residue with a less polar solvent to obtain intermediate M1, the reaction formula is as follows. The preparation process provided by the invention has simple operation steps, mild reaction conditions, simpler post-treatment required for the reaction, greatly improved product yield and purity, effectively reduces the generation of 2-substituted impurities, and is better for the promotion and improvement of palbocoxib technology. It is of great significance to be used in clinical patients.

The invention provides a simple preparation method of palbociclib. The method comprises the steps: performing dehydration on an acetacetate under the action of an acid catalyst so as to prepare 2-acetyl-3-methyl-2-pentenediate diester (II), then performing amidation condensation on the 2-acetyl-3-methyl-2-pentenediate diester (II) and cyclopentylamine so as to prepare 3-acetyl-1-cyclopentyl-4-methylpyridine-2,6-(1H,5H)-dione (III), then performing condensation on 3-acetyl-1-cyclopentyl-4-methylpyridine-2,6-(1H,5H)-dione (III) and a methylenation reagent so as to prepare 3-acetyl-1-cyclopentyl-4-methyl-5-dialkylaminomethylenepyridine-2,6-(1H,5H)-dione (IV), then performing a pyrimidine cyclization reaction on the 3-acetyl-1-cyclopentyl-4-methyl-5-dialkylaminomethylenepyridine-2,6-(1H,5H)-dione (IV) and N-[5-(4-tert-butoxycarbonylpiperazin-1-yl)pyridin-2-yl]guanidine (V) so as to obtain Boc-protected palbociclib (VI), and removing a Boc protecting group so as to obtain the palbociclib (I). The method has the advantages of a short process, simple operation, easy realization, low cost, less waste, high product purity and high yield.

The invention discloses a preparation method of a palbociclib intermediate, which uses 5-bromo-2,4-dichloropyrimidine and cyclopentylamine, uses dichloromethane and other solvents and water as solvents, and uses inorganic bases as acid-binding Preparation of 5-bromo-2-chloro-N-cyclopentaline-4 amine, then DIEA is used as an acid-binding agent, DMF is a solvent, and TBAB is a phase transfer catalyst. In the presence of water, a small amount of palladium is used to catalyze, Through normal hexane reflux dehydration, further dehydration ring closure of acetic anhydride obtains 2-chloro-8-cyclopentyl-5-picoline [2,3-D] pyrimidin-7 (8H)-one, the obtained compound is in acetonitrile In reaction with NBS, 6-bromo-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-D]pyrimidin-7(8H)-one is obtained. The method has the advantages of mild reaction, simple and convenient operation, reusable solvent, less environmental pollution, high yield, low cost and high product quality, and is suitable for industrialized production.

The invention relates to platinum (IV) anticancer compounds with a dihydrogen phosphate radical as an axial ligand. The chemical structure of the compounds is shown in the description. In the structure, a carrier group 2A is an ammonia / amine liand, and comprises 2NH3, 1R,2R-cyclohexanediamin, 1,2-bis(aminomethyl)cyclobutane, NH3 / cyclopentamine and NH3 / cyclohexylamine; and leaving groups 2X are the leaving groups of platinum (II) anticancer compounds existing at present, and comprise 2Cl<->, an oxalate radical, a 1,1-cyclobutanedicarboxylate radical and a propane dicarboxylate radical. Phosphoric acid bonding is helpful for running of compounds to cancer cell nuclei, improving the selectivity of cancer cells, and makes the compounds mediate compound targeting osteocarcinoma and have very strong anticancer effect. The compounds have the advantages of good water solubility and stability, and are highly suitable for being used as anticancer drugs.

The present invention relates to the fields of pharmaceutical chemistry and pharmaceutical therapeutics. Provided are an amino-substituted rutaecarpin analog and a synthesis method and use thereof in the preparation of an anti-obesity drug. An experiment confirms that the amino-substituted rutaecarpin analog of the present invention can dramatically reduce the lipopexia of 3T3-L1 fat cells, and can reduce the high levulose-induced lipopexia of FAO rat liver cells. A cellular level experiment indicates that the compound can reduce lipopexia, relieve obesity and alleviate fatty liver. The amino-substituted rutaecarpin analog has a chemical formula (I), wherein R0=-NH(CH2)nR2, n=1, 2, 3, 4 or 5, and R2=-N(CH3)2, -N(CH2CH3)2, cyclopentylamino or cyclohexylamino; or R0= morpholinyl, piperazinyl or methylpiperazinyl.

The invention belongs to the technical field of biomedicine, in particular to a cyclohexane amine D 3 / D 2 Receptor partial agonist and its pharmaceutically acceptable salt, its synthesis method and application. Compared with the prior art, the N-fluorocyclic carbamoyl group connected by cyclopentylamine in the molecular structure provided by the present invention has stronger metabolic stability than the original N,N-dimethylcarbamoyl group, prolonging the drug In vivo action time. The introduction of the fluorinated cyclic amino group changes the physical and chemical properties of the original molecule, thereby changing the pharmacokinetic properties, enhancing the distribution of the drug in the target tissue, and improving the bioavailability of the drug. The inventors also surprisingly found that the introduction of the fluorinated cyclic amino group affects the local conformation of the compound, enhances the mutual binding ability between the ligand and the target protein, and improves the selectivity of the target.