32 results about "Ponatinib" patented technology

The invention relates to a preparation method of a drug for treating chronic granulocytic leukemia, belonging to the field of medical chemistry, and specifically relates to a preparation method of 3-[2-(imidazo[1,2-b] pyridazine-3-yl) acetenyl]-4-methyl-N-{4-[4-methyl piperazine-1-yl] methyl}-3- trifluoromethyl phenyl} benzoyl amide (ponatinib). The method comprises the following steps: adding a phosphine ligand and cesium carbonate at the same time by taking Pd(PPh3)2Cl2 as a catalyst; adding strong base DBU or adding CuI as a cocatalyst to carry out sonagashira reaction, wherein the phosphine ligand is selected from tricyclohexyl phosphine (PCy3), tri-tert-butyl phosphine (PtBu3) or tri(funan-2-yl) phosphine (P(2-furyl)3). The method disclosed by the invention is complete in reaction, does not have or has extremely few diyne byproduct of alkyne coupling, and is easy to separate and purity.

The invention discloses a preparing method of ponatinib. The preparing method of ponatinib comprises the steps of building a reaction system in copper salt and alkaline organic solvent with 3-halogen-parazole [1,5-a]pyrimidine being the starting point, with trimethylsilylacetylene, tetrabutylammonium fluoride and the like being raw materials in sequence and with acridine salt being a photocatalyst, and thus indirectly building a synthesizing path of ponatinib. The synthesis conditions are mild, the cost is low, and the yield of ponatinib is high.

The invention discloses a preparation method for Ponatinib (I). The preparation method comprises the following steps: imidazo [1, 2-b] pyridazine-3-formyl chloride (II) is used as a raw material and subjected to the Friedel-Crafts acylation reaction with 4-methyl benzoic acid (III) to generate an intermediate (IV) being 3-(imidazo[1, 2-b] pyridazine-3-yl)-(4-methyl benzoic acid-3-yl) ketone, the intermediate (IV) is subjected to the Omair-Amos reaction with a Wittig reagent under alkaline condition to obtain an intermediate (V) being 3-(imidazo[1, 2-b] pyridazine-3-ethynyl)-4-methyl benzoic acid, the intermediate (V) is subjected to the amidation reaction with side chain (VI) being 4-((4-methyl piperazine-1-yl)-methyl)-3-(trifluoromethyl) aniline to obtain the Ponatinib (I). According to the preparation method provided by the invention, the raw materials are easy to obtain, the process is concise, and the method is economical and environment-friendly and is suitable for industrial production.