121 results about "Pyrimidifen" patented technology

The present disclosure provides a method of regioselective synthesis of an imidazo-pyrimidine compound of formula (XXa) or (XXb), the method comprising the step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2. The cyclization reaction of imidazo [1, 2-a] pyrimidine-amine generated between beta-ethoxy acrylamide and phosphorylated aminoimidazole depends on the guiding effect from the phosphorylated aminoimidazole in the ring and the phosphorylated aminoimidazole outside the ring. According to the reaction, the 2-amino or 4-amino structure isomer of the imidazo [1, 2-a] pyrimidine is generated in a good yield and a regioselectivity range of 90: 10 to 99: 1. The reactions can be used to synthesize a variety of tracer molecules for neurological condition research, such as where R3 and R4 together with the imidazole ring atom to which they are bonded form a benzene ring, and the product is a substituted benzimidazopyrimidine. The reaction may be summarized to form imidazo [1, 2-a] pyrimidines substituted at its 2-and 4-positions with alkoxy or thioalkyl groups.

The invention provides a preparation method of a tofacitinib impurity, and relates to the field of drug synthesis and drug quality research. The preparation method comprises the steps of dissolving N-methyl-N-((3R, 4R)-4-methylpiperidine-3-yl)-7H-pyrrolo [2, 3-d] pyrimidine-4-amine dihydrochloride in a first organic solvent, and reacting with methyl 3-chloro-3-oxopropionate under the catalysis of an acid-binding agent to obtain 3-((3R, 4R)-4-methyl-3-(methyl (7H-pyrrolo [2, 3-d] pyrimidine-4-yl) amino) piperidine-1-yl)-3-oxopropionic acid methyl ester,dissolving the product in a second organic solvent, adding an alkaline reagent, and adjusting the pH value to be acidic, thereby obtaining the tofacitinib impurity. The tofacitinib impurity is 3-((3R, 4R)-4-methyl-3-(methyl (7H-pyrrolo [2, 3-d] pyrimidine-4-yl) amino) piperidine-1-yl)-3-oxopropionic acid. The method is simple, and the product is high in yield and purity.

The present invention discloses a compound used as a general formula (I) of protein kinase inhibitor, the salt accepted pharmaceutically and the preparation method; wherein, X is -(CH2)m-COO-; m is equal to 1 to 5 or direct bond; Y is -(CH2)n-O- or -(CH2)n-PhO-; n is equal to1 to 10 or direct bond; the preparation method comprises a step which uses N-(5-amino-2- methyl-phenyl)-4- (3-pyridyl)-2-pyrimidinamine and general formula (II) compound as raw material synthesis. The present invention also discloses the preparation method of the compound, comprising the compound and the treatment of being used as tyrosine protein kinase inhibitor in diseases such as cancer relative to tyrosine in particular to Bcr-Abl.

A Preparation method of pyrazolo[3,4-d]pyrilamine compounds comprises the following steps: allowing phosphinimine prepared by pyrazole compounds with cyans and aminos at an ortho-position to react with various isocyanates by an aza-witting reaction under a mild condition in dichloromethane to obtain carbodiimide, then performing a cyclization reaction with alcohol in solvent alcohol with sodium hydroxide as an alkali so as to efficiently prepare the pyrazolo[3,4-d]pyrilamine compounds through a series process. The method of the invention is mild in reaction condition, wide in substrate application scope (R1=H or various electron-donating groups such as CH3, OCH3, OC2H5, and the like, or various electron-withdrawing groups such as 4-Cl, 4-F, and the like, wherein R2 is methanol or ethanol), less in side reaction, high in product purity, and convenient for separation and purification; the method is convenient for operation, low in cost, suitable for large-scale preparation, and has very good application prospects.