72 results about "Pitavastatine" patented technology

The invention discloses a synthesis method of pitavastatin tert-butyl ester, which comprises the following steps: carrying out a reaction on (4R-Cis)-6-chloromethyl-2,2-dimethyl-1,3-dioxolane-4-tert-butyl acetate with a substance A under the action of a first base catalyst to obtain a substance B; oxidizing the substance B with an oxidizing agent to obtain a substance C; carrying out a reaction with 2-Cyclopropyl-4-(4-fluorophenyl)-quinoline-3-formaldehyde under the action of a second base catalyst to obtain a substance D; and finally, performing acid deprotection to obtain the pitavastatin tert-butyl ester. The method has the advantages of mild and controllable reaction conditions, wherein the reaction conditions of Julia olefination are free of requirement of ultralow-temperature reaction, so that the synthesis method has advantages of convenience and simplicity in operation, good stereoselectivity and high yield, and the synthesized pitavastatin tert-butyl ester is completely free of cis-isomer and high in purity.

The invention relates to a method for preparing high-optical purity pitavastatin calcium. The method comprises the following steps of: deprotecting (3R,5S)-dyhydroxyl-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dyhydroxyl-3,5-Oisopropylidene-6-tert-butyl heptenoate (I) serving as an initial raw material by using acid, and removing impurities under a certain pH value; adding excessive D-(+)benzyl methylamine, and crystallizing to extract heptenoic acid amine salt (IV); and adding calcium chloride to obtain the pitavastatin calcium. The method has the advantages that the reaction condition is mild, the purity of the product is high, the optical purity is more than or equal to 99.5 percent, the yield is more than or equal to 50 percent, the problems of high difficulty of separation and purification and low yield in the conventional method for synthesizing the pitavastatin calcium, and the method is suitable for industrialization.

The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma.The present invention relates to a prophylactic and / or therapeutic agent for hyperlipidemia, a prophylactic and / or therapeutic agent for obesity or diabetes mellitus, and a prophylactic and / or therapeutic agent for metabolic syndrome, each agent including a compound represented by the formula (1), or a salt thereof, and a statin, particularly pitavastatin, in combination.

The invention relates to a pharmaceutical composition containing rosuvastatin or pitavastatin compounds and B vitamins; wherein the content of rosuvastatin or pitavastatin compounds is 1-40 mg, and the content of B vitamins is 0.1-50 mg . The invention also provides the application of the pharmaceutical composition in the preparation of medicines for preventing, treating and delaying atherosclerosis and related cardiovascular and cerebrovascular diseases. The invention has the advantages that the curative effect of the statin lipid-lowering drugs can be improved, the vascular endothelial protection and anti-atherosclerosis aspects are superior to the statin lipid-lowering drugs, the side effects of the statin lipid-lowering drugs are reduced, and the toxicity is not increased, In addition, it can make it convenient for patients to take medicines and reduce medical expenses.

Production of pitavastatin calcium safely on an industrial scale with a high yield and high selectivity at low cost. A method of producing pitavastatin calcium including step (i) for acetalizing a compound represented by the formula (1) to give a compound represented by the formula (3), step (ii) for reacting a compound represented by the formula (3) with an acid to give a compound represented by the formula (4), and step (iii) for hydrolyzing a compound represented by the formula (4) and reacting same with a calcium compound.

The present invention relates to a kind of preparation method of pitavastatin calcium intermediate [[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl] methyl] triphenylphosphine bromide, comprising the following Said steps: make 2-cyclopropyl-4-(4-fluorophenyl)-3-quinoline methanol and triphenylphosphine hydrobromide react in an organic solvent to obtain the target compound. The preparation method of the invention has easy-to-obtain raw materials, simple operation and high yield, effectively reduces phosphorus-containing waste water and phosphorus-containing waste residue, reduces production costs, and is beneficial to large-scale production.

The present invention provides a pharmaceutical product which includes a solid preparation comprising pitavastatin or a salt thereof, in which production of a lactone form thereof is suppressed.The pharmaceutical product is characterized by including a solid preparation comprising the following ingredients (A) and (B): (A) pitavastatin or a salt thereof; and (B) at least one member selected from the group consisting of carmellose and a salt thereof, crospovidone, and microcrystalline cellulose, and the solid preparation having a water content of 2.9 mass % or less, wherein the solid preparation is stored in a tight package.

The invention discloses a refining method of pitavastatin tert-butyl ester, which comprises the following steps: cooling and crystallizing a mixed solvent in which pitavastatin tert-butyl ester raw materials are dissolved, filtering, and drying; wherein, the mixed solvent It is a mixture of methyl tert-butyl ether and non-polar organic solvent; the non-polar organic solvent is n-hexane, n-heptane, cyclohexane, n-pentane, cyclopentane, octane or isooctane. According to the refining method of the present invention, the isomer content in the obtained pitavastatin tert-butyl ester is low, and the refining effect is good. Epimer impurity 1, epimer impurity 2 and enantiomer impurity The contents are all below 0.05%. Moreover, the refining method of the present invention has high yield, low uncontrollability, simple operation, is suitable for large-scale industrial production, and can prepare high-purity pitavastatin calcium.