METHOD OF ROSUVASTATIN CALCIUM SALT PREPARATION Russian patent published in 2008 - IPC C07D239/42 

Abstract RU 2326871 C2

FIELD: chemistry.

SUBSTANCE: invention refers to the improved method of the preparation of calcium salt (E)-7-[4-(4-phtorphenyl)-6-isopropyl-2-[methyl(mesyl) amino]pyrimidine-5] (3R,5S)- 3.5-dihydroxyhepten-6 acid (rosuvastin),adding chloride solution into water soluble salt solution (E)-7-[4-(4-phtorphenyl)-6-isopropyl-2-[methyl(mesyl) amino]pyrimidine-5] (3R,5S)- 3.5-dihydroxyhepten-6 acid at 30-45°C temperature. Preferable time of addition is 5-60 minutes. After adding calcium chloride, the mixture is blended usually during ageing time at least 10 minutes at 30-45°C, filtered, if it is necessary the mixture is flushed out, the prepared product is dried. The temperature of the mixture during ageing should be equal to the temperature of addition. Moreover the temperature and time of addition, duration of addition are regulated in such way that to get the product with specific surface less or equal 1m/g (if the Fisher's method is used), preferably, to get the product with specific surface less or equal 0.5 m2/g (if the Fisher's method is used). The end product has the paste concentration of more than about 45% weight ratio. The paste concentration of the product is at least 50% of weight ratio after maximum 15 minutes of filtration by laboratory scale. Preferably, to prepare the product with the paste concentration more than about 70% weight ratio. Alcali salt can be used as water soluble salt solution (E)-7-[4-(4-phtorphenyl)-6-isopropyl-2-[methyl(mesyl) amino]pyrimidine-5] (3R,5S)- 3.5-dihydroxyhepten-6 acid, for example sodium salt or ammonium salt, methylamine salt or tris (tris(hydroxymethyl)aminomethane) salt.

EFFECT: salt is prepared by means of treating of acid or its salt with the corresponded base.

27 cl, 1 tbl, 4 ex

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RU 2 326 871 C2

Authors

Khorberi Dzhon

Tejlor Najdzhel Filip

Dates

2008-06-20Published

2003-08-07Filed