Olaparib refining method

Abstract

The invention discloses an olaparib refining method, which comprises: (1) dissolving an olaparib crude product in a mixed solvent of ethyl acetate and acetone, and controlling the temperature at 45-50DEG C until olaparib is completely dissolved; (2) adding active carbon, decolorizing, filtering, cooling the filtrate to a temperature of -10-0 DEG C, crystallizing, and growing the crystal; and (3)filtering, washing the filtered solid by using acetone, and carrying out vacuum drying to obtain the refined olaparib. With the refining method of the present invention, the purity of the obtained olaparib can reach more than 99.9%, the total impurity and the single impurity are respectively controlled within 0.1% and 0.05%, the quality of the product is remarkably improved, the refining process is easy to operate, and the refining method is suitable for industrial production.

Description

Technical field

[0001] The invention belongs to the technical field of medicine, and specifically relates to a method for refining the anti-tumor drug olaparib. Background technique

[0002] Olapani was first developed by the British biotechnology company KuDOS (Kudos) Pharmaceuticals Co., Ltd., and is an oral polyadenylic acid diphosphate ribose transferase (PARP) inhibitor. It mainly blocks the repair of DNA damage, causes the accumulation of DNA damage, and ultimately kills tumor cells; in addition, it can increase the sensitivity of cells to other endogenous and exogenous DNA damage factors; inhibit angiogenesis; enhance the immunity of normal cells, thereby Resist the invasion of cancer cells.

[0003] The therapeutic effect of olaparib on ovarian cancer has been highly recognized. EMEA and FDA have successively granted orphan drug certification for olaparib to treat ovarian cancer.

[0004] The chemical name of olaparib is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-...

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