Process for preparing irinotecan hydrochloride medicines

A technology for irinotecan hydrochloride and drugs, which is applied in the field of preparation of irinotecan hydrochloride drugs, can solve the problems of large solvent demand, low efficiency, and impure products, and achieve improved production efficiency, high product purity, and simple operation Effect

Inactive Publication Date: 2008-02-27
SICHUAN XIELI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

The products in each step of this process are impure, and the most critical intermediate of irinotecan, 7-ethyl-10-hydroxycamptothecin, has a very low purity, only about 80-85%. In order to synthesize irinotecan hydrochloride, a very complicated process is required. Column chromatography process, which greatly increases the difficulty of synthesis of irinotecan
Moreover, the photoreaction is difficult to control, the demand for solvent is large, the efficiency is low, and it is difficult to achieve large-scale production
Impurities related to irinotecan hydrochloride produced by this process cannot reach below 0.1%

Method used

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  • Process for preparing irinotecan hydrochloride medicines
  • Process for preparing irinotecan hydrochloride medicines

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Experimental program
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Embodiment Construction

[0019] The preparation method of the present embodiment irinotecan hydrochloride medicine comprises the steps:

[0020] 1) Camptothecin ethylation reaction to obtain 7-ethylcamptothecin;

[0021] 2) Hydrogenation of 7-ethylcamptothecin to obtain hydrogenated-7-ethylcamptothecin;

[0022] 3) Oxidation of hydrogenated-7-ethylcamptothecin to obtain 7-ethyl-10-hydroxycamptothecin;

[0023] 4) Coupling reaction of 7-ethyl-10-hydroxycamptothecin and 4-piperidinylpiperidinecarbonyl chloride to prepare irinotecan hydrochloride.

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Abstract

The invention discloses a making method of alcaine yilitikang drug, which comprises the following steps: 1) ethylizing camptothecine to produce 7-ethyl camptothecine; 2) hydrogenating the 7-ethyl camptothecine; obtaining hydrogenated-7-ethyl camptothecine; 3) oxidizing the hydrogenated-7-ethyl camptothecine to produce 7-ethyl-10-hydroxy camptothecine; 4) coupling the 7-ethyl-10-hydroxy camptothecine and 4-piperidine radical piperidine formyl chloride to obtain the product with simple operation, high efficiency, high receiving rate, lost and high quality.

Description

Technical field: [0001] The present invention relates to the preparation method of irinotecan hydrochloride medicine. technical background: [0002] Irinotecan (CPT-11) is a camptothecin derivative isolated from natural plants. It is a water-soluble anti-tumor raw material drug and a broad-spectrum tumor drug recently listed abroad. For the treatment of tumors, advanced colon cancer, rectal cancer, small cell lung cancer, cervical cancer, ovarian cancer and non-Hodgkinson's lymphoma. When used in combination with other anti-tumor drugs, the anti-tumor effect can be enhanced and the toxicity can be reduced. [0003] Irinotecan is one of the new drugs in the camptothecin class. In 1966, Wall et al. extracted camptothecin, a substance with anti-tumor activity, from the Chinese plant camptothecin, but due to its poor water solubility and unpredictable severe toxicity , limiting the further application of camptothecin. Until the 1980s, it was found that camptothecin is a DNA t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/22
Inventor 张强
Owner SICHUAN XIELI PHARM CO LTD
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