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Preparation method of medicine Olaparib for treating ovarian cancer

A technology for ovarian cancer and drugs, which is applied in the field of drug preparation, can solve the problem of no removal of special impurities in double-substituted products, and achieve the effect of reduced hygroscopicity and good removal effect

Inactive Publication Date: 2017-11-24
HUNAN QIWEI TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Although the above preparation method has a good scavenging effect on most of the impurities in olaparib, it has almost no scavenging effect on the special impurity of the double-substituted product. Therefore, it is necessary to develop a new preparation method to obtain high-purity olaparib. Rapani

Method used

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  • Preparation method of medicine Olaparib for treating ovarian cancer
  • Preparation method of medicine Olaparib for treating ovarian cancer
  • Preparation method of medicine Olaparib for treating ovarian cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Add 10 g of crude olaparib to 70 mL of a mixed solvent of dimethyl carbonate and isopropyl ether (the volume ratio of dimethyl carbonate and isopropyl ether is 1.0:1), and slowly heat to 45-50° C. Keep stirring at a stirring speed of 110 rpm for 30 minutes, continue to heat up to 60-65°C, stir at a stirring speed of 110 rpm for 30 minutes, dissolve the crude product, and obtain a crude product solution; add activated carbon to the crude product solution, decolorize, filter, and collect the filtrate Slowly lower the temperature, reduce the temperature of the filtrate to 30-35°C, keep warm, control the stirring speed at 110 rpm, and stir for 30 minutes; then cool the filtrate to 5°C or below, control the stirring speed at 150 rpm, and add 0.2g of seed crystals , after controlling the temperature and stirring speed at 150 revs / min to grow the crystal for 2 h, filter, filter the cake with a small amount of dimethyl carbonate and isopropyl ether mixed solvent rinse, suction f...

Embodiment 2

[0033] Add 10 g of crude olaparib to 75 mL of a mixed solvent of dimethyl carbonate and isopropyl ether (the volume ratio of dimethyl carbonate and isopropyl ether is 1.2:1), slowly heat to 45-50 ° C, and Keep stirring at a stirring speed of 110 rpm for 30 minutes, continue to heat up to 60-65°C, stir at a stirring speed of 110 rpm for 30 minutes, dissolve the crude product, and obtain a crude product solution; add activated carbon to the crude product solution, decolorize, filter, and collect the filtrate Slowly lower the temperature, reduce the temperature of the filtrate to 30-35°C, keep warm, control the stirring speed at 110 rpm, and stir for 30 minutes; then cool the filtrate to 5°C or below, control the stirring speed at 150 rpm, and add 0.2g of seed crystals , after controlling the temperature and stirring speed at 150 revs / min to grow the crystal for 2 h, filter, filter the filter cake with a small amount of dimethyl carbonate and isopropyl ether mixed solvent rinse, s...

Embodiment 3

[0036] Add 10 g of crude olaparib to 80 mL of a mixed solvent of dimethyl carbonate and isopropyl ether (the volume ratio of dimethyl carbonate and isopropyl ether is 1.5:1), and slowly heat to 45-50° C. Keep stirring at a stirring speed of 110 rpm for 30 minutes, continue to heat up to 60-65°C, stir at a stirring speed of 110 rpm for 30 minutes, dissolve the crude product, and obtain a crude product solution; add activated carbon to the crude product solution, decolorize, filter, and collect the filtrate Slowly lower the temperature, reduce the temperature of the filtrate to 30-35°C, keep warm, control the stirring speed at 110 rpm, and stir for 30 minutes; then cool the filtrate to 5°C or below, control the stirring speed at 150 rpm, and add 0.2g of seed crystals , after controlling the temperature and stirring speed at 150 revs / min to grow the crystal for 2 h, filter, filter the cake with a small amount of dimethyl carbonate and isopropyl ether mixed solvent rinse, suction f...

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Abstract

The invention relates to a preparation method of medicine Olaparib for treating ovarian cancer. The preparation method comprises the following steps of 1, adding Olaparib crude product into mixed solvent of dimethyl carbonate and isopropyl ether, slowly heating to 45-50 DEG C, keeping warm and stirring for 30min, continuously raising to 60-65 DEG C, stirring until the crude product is dissolved to acquire crude production solution; 2, adding active carbon, into the crude product solution, decoloring, filtering and collecting filtrate; 3, slowly cooling to reduce the temperature of the filtrate to 30-35 DEG C, keeping warm and stirring; and 4, further cooling the filtrate to be 5 DEG C and below, controlling a stirring speed to be 150 turns / min, adding seed crystal, filtering after controlling the temperature and the steering speed to grow the crystal for 2h, washing a filter cake with a small amount of mixed solvent of dimethyl carbonate and isopropyl ether, and drying to acquire the Olaparib. The preparation method provided by the invention is simple in technology, high in yield and purity, particularly significantly reduced in bisubstituted product, and meanwhile an applicant is surprised to find that the prepare Olaparib is significantly reduced in hygroscopicity.

Description

technical field [0001] The invention relates to a preparation method of a known medicine, in particular to a preparation method of olaparib, belonging to the technical field of medicine preparation. Background technique [0002] Olaparib, the chemical name is 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one, the English name is Olaparib, and the structural formula is as follows Formula 1 shows: [0003] [0004] Olaparib, a small molecule developed by KuDOS Pharmaceuticals, a wholly owned subsidiary of AstraZeneca, is a potent PARP inhibitor that promotes tumor Apoptosis, which can enhance the efficacy of radiotherapy and chemotherapy with alkylating agents and platinum drugs, and is mainly used for the treatment of breast cancer gene 1 or 2 (BRCA-1 or BRCA-2) gene mutation cancer (mainly present in the breast cancer, ovarian and prostate cancer). Olaparib can selectively act on tumor cells, and normal cells are not destroyed due t...

Claims

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Application Information

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IPC IPC(8): C07D237/32
CPCC07D237/32
Inventor 朱社凤
Owner HUNAN QIWEI TECH CO LTD
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