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Preparation method of capecitabine

A capecitabine and flucytosine technology, applied in the field of drug preparation, can solve problems such as high price, achieve the effects of reducing production cost and consumption, solving environmental pollution, and being easy to control

Inactive Publication Date: 2014-12-17
上海宏冠医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, since the raw material used is 5-fluorouridine, which is expensive, this route has similar defects to the aforementioned route, and it is taboo to use in large-scale industrial production.

Method used

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  • Preparation method of capecitabine
  • Preparation method of capecitabine

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Embodiment Construction

[0013] 1. Add 60ml (0.46mol) of n-pentyl carbonate, 5ml of DMF, and 60ml of dichloromethane to the reactor in turn, stir, cool to 0°C, and dropwise add 60.3g (0.51mol) of thionyl chloride + 60ml of dichloromethane to form solution, control the dropping temperature at -2-0°C, after dropping, keep warm for 2-3 hours. Add 20ml of water, stir to remove the water layer, add 38g (0.3mol) of 5-fluorocytosine and 30ml of triethylamine to the organic layer, stir and react at room temperature for 4 hours, add 30ml of water, stir to remove the water layer, organic layer Dry over anhydrous magnesium sulfate, remove the solvent, and obtain 79.4 g of a white solid product, which is directly used in the next step without refining;

[0014] 2. Stir 44.1g (0.35mol) of anhydrous manganese chloride, 67.6g (0.26mol) of 1,2,3-triacetyl-5-deoxy-D-ribose and 200ml of dichloromethane to form a solution, then cool to 0°C Prepare as follows; add 100ml of toluene, 15.9ml of hexamethyldisilazane, and 9....

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Abstract

The invention provides a preparation method of capecitabine. The method comprises the following steps: reacting n-amyl formate and 5-flucytosine to prepare an amide derivative of 5-flucytosine, then reacting with 1,2,3-triacetyl-5-deoxy-D-ribose to obtain a product, and performing alkaline hydrolysis to the obtained product to obtain capecitabine. The method has the advantages of convenient material control and lower cost; and manganese chloride is used in the condensation process and manganese can be reused after being recycled, thus the environmental pollution problem of the existing preparation method can be solved.

Description

technical field [0001] The invention relates to a medicine preparation process, in particular to a preparation method of capecitabine. Background technique [0002] Capecitabine (capecitabine) was developed by the Swiss pharmaceutical company Roche (Roche), and was marketed in the United States, Canada, Sweden and other countries under the trade name Xeloda in 1998. At present, my country has approved the import of this product, which is clinically used in the treatment of advanced breast cancer, colorectal cancer and other solid tumors. Capecitabine is an oral cytotoxic agent with selective activity against tumor cells. As an oral drug activated in tumors, capecitabine has high anti-tumor selectivity and strong specificity. After oral administration, capecitabine is completely absorbed through the gastrointestinal tract, undergoes a unique 3-step activation mechanism, and finally converts into 5-fluorouracil (FU) after reaching the tumor tissue to exert cytotoxicity, so i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/06C07H1/00
Inventor 杨继斌方晏燕贺学林史命锋叶澜杰孙国建龚海燕李洪文
Owner 上海宏冠医药科技有限公司
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