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Olaparib compound and preparation method thereof

A technology of olaparib and its compound, which is applied in the field of olaparib compound and its preparation, can solve problems such as inability to break through, and achieve the effects of improved solubility, improved dissolution rate and stability, and good stability

Inactive Publication Date: 2017-09-15
SHANDONG YUXIN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The poor solubility of olaparib raw materials has always been a technical difficulty in this field, and has been unable to break through

Method used

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  • Olaparib compound and preparation method thereof
  • Olaparib compound and preparation method thereof
  • Olaparib compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1: Preparation of olaparib compound

[0050] (1) Get 100 g of the crude product of olaparib, add 1500 ml of mixed solvent of chloroform / petroleum ether (0.5:1 by volume), stir and heat at 200 rpm until completely dissolved, decolorize activated carbon, and filter;

[0051] (2) Reduce the filtrate of step (1) from 3°C to 10°C every 10 minutes, add 1500ml of ethanol dropwise at 1.5mL / min, and continue to cool down to -5°C every 10 minutes to crystallize;

[0052] (3) Insulate and stir until the crystallization is complete, grow the crystal for 2 hours, filter with suction, wash with water, and dry at 40°C to obtain 99.92g of white crystalline powder with a yield of 99.92% and a purity of 99.99%.

[0053] The X-ray powder diffraction spectrogram that the prepared white crystalline powder uses Cu-Kα ray measurement to obtain is shown in figure 1 .

Embodiment 2

[0054] Embodiment 2: Preparation of olaparib compound

[0055] (1) Get 100 g of the crude product of olaparib, add 1000 ml of mixed solvent of chloroform / petroleum ether (1:1 by volume), stir and heat at 200 rpm until completely dissolved, decolorize activated carbon, and filter;

[0056] (2) Reduce the filtrate of step (1) from 4°C to 10°C every 10 minutes, add 1200ml of ethanol dropwise at 2.0mL / min, and continue to cool down from 3°C to -3°C every 10 minutes to crystallize;

[0057] (3) Insulate and stir until crystallization is complete, grow crystals for 2.5 hours, filter with suction, wash with water, and dry at 45°C to obtain 99.91g of white crystalline powder with a yield of 99.91% and a purity of 99.98%.

[0058] The X-ray powder diffraction spectrum obtained by measuring the prepared white crystalline powder using Cu-Kα rays is similar to that of Example 1.

Embodiment 3

[0059] Embodiment 3: Preparation of olaparib compound

[0060] (1) Get 100g of the crude product of olaparib, add 1200ml of mixed solvent of chloroform / petroleum ether (1:1 by volume), stir and heat at 200 rpm until completely dissolved, decolorize activated carbon, and filter;

[0061] (2) Reduce the filtrate of step (1) from 2°C to 10°C every 10 minutes, add 1320ml of ethanol dropwise at 1.0mL / min, and continue to cool down from 3°C to 0°C every 10 minutes to crystallize;

[0062] (3) Insulate and stir until crystallization is complete, grow crystals for 3 hours, filter with suction, wash with water, and dry at 40°C to obtain 99.89g of white crystalline powder with a yield of 99.89% and a purity of 99.99%.

[0063] The X-ray powder diffraction spectrum obtained by measuring the prepared white crystalline powder using Cu-Kα rays is similar to that of Example 1.

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Abstract

The present invention belongs to the technical field of medicine, and discloses an olaparib compound and a preparation method thereof, wherein the olaparib of the present invention has advantages of high purity and good stability, and has characteristic diffraction peaks in the X-ray powder diffraction pattern when the 2[theta]+ / -0.2 DEG C diffraction angle is 4.2679 DEG, 10.1345 DEG, 12.6058 DEG, 15.3421 DEG, 18.6022 DEG, 19.8103 DEG, 22.9050 DEG and 25.2146 DEG, and the X-ray powder diffraction pattern obtained through Cu-K[alpha] ray measurement is represented by Fig. 1 and is completely different from the X-ray powder diffraction pattern in the prior art. The experiment results show that the obtained olaparib has significantly improved solubility. The invention further discloses a preparation method of the olaparib, wherein the preparation method has advantages of simple and easy operation, high yield, high product purity and mild reaction conditions, and is suitable for large-scale production. The dissolution and the stability of the capsules prepared from the olaparib of the present invention are remarkably improved, and the obtained capsules are suitable for clinical use.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an olaparib compound and a preparation method thereof. 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 to the retention of the double-strand repair func...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/32A61K31/502A61K9/48A61P35/00
CPCC07D237/32A61K9/48C07B2200/13
Inventor 李华刘纯海巩腾文
Owner SHANDONG YUXIN PHARMA CO LTD
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